Assay ID | Title | Year | Journal | Article |
AID1345682 | Human BLK proto-oncogene, Src family tyrosine kinase (Src family) | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies. |
AID1345572 | Human erb-b2 receptor tyrosine kinase 4 (Type I RTKs: ErbB (epidermal growth factor) receptor family) | 2016 | The New England journal of medicine, Jan-28, Volume: 374, Issue:4
| Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia. |
AID1345682 | Human BLK proto-oncogene, Src family tyrosine kinase (Src family) | 2016 | The New England journal of medicine, Jan-28, Volume: 374, Issue:4
| Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia. |
AID1345705 | Human IL2 inducible T cell kinase (Tec family) | 2016 | The New England journal of medicine, Jan-28, Volume: 374, Issue:4
| Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia. |
AID1345882 | Human tec protein tyrosine kinase (Tec family) | 2016 | The New England journal of medicine, Jan-28, Volume: 374, Issue:4
| Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia. |
AID1345597 | Human FYN proto-oncogene, Src family tyrosine kinase (Src family) | 2016 | The New England journal of medicine, Jan-28, Volume: 374, Issue:4
| Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia. |
AID1345717 | Human LCK proto-oncogene, Src family tyrosine kinase (Src family) | 2016 | The New England journal of medicine, Jan-28, Volume: 374, Issue:4
| Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia. |
AID1345617 | Human Bruton tyrosine kinase (Tec family) | 2016 | The New England journal of medicine, Jan-28, Volume: 374, Issue:4
| Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia. |
AID1345861 | Human SRC proto-oncogene, non-receptor tyrosine kinase (Src family) | 2016 | The New England journal of medicine, Jan-28, Volume: 374, Issue:4
| Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia. |
AID1345502 | Human epidermal growth factor receptor (Type I RTKs: ErbB (epidermal growth factor) receptor family) | 2016 | The New England journal of medicine, Jan-28, Volume: 374, Issue:4
| Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia. |
AID1345664 | Human BMX non-receptor tyrosine kinase (Tec family) | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies. |
AID1345654 | Human HCK proto-oncogene, Src family tyrosine kinase (Src family) | 2016 | The New England journal of medicine, Jan-28, Volume: 374, Issue:4
| Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia. |
AID1345617 | Human Bruton tyrosine kinase (Tec family) | 2007 | ChemMedChem, Jan, Volume: 2, Issue:1
| Discovery of selective irreversible inhibitors for Bruton's tyrosine kinase. |
AID1345849 | Human YES proto-oncogene 1, Src family tyrosine kinase (Src family) | 2016 | The New England journal of medicine, Jan-28, Volume: 374, Issue:4
| Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia. |
AID1345860 | Human TXK tyrosine kinase (Tec family) | 2016 | The New England journal of medicine, Jan-28, Volume: 374, Issue:4
| Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia. |
AID1345664 | Human BMX non-receptor tyrosine kinase (Tec family) | 2016 | The New England journal of medicine, Jan-28, Volume: 374, Issue:4
| Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia. |
AID1345653 | Human erb-b2 receptor tyrosine kinase 2 (Type I RTKs: ErbB (epidermal growth factor) receptor family) | 2016 | The New England journal of medicine, Jan-28, Volume: 374, Issue:4
| Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia. |
AID1345744 | Human Janus kinase 3 (Janus kinase (JakA) family) | 2016 | The New England journal of medicine, Jan-28, Volume: 374, Issue:4
| Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia. |
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. |
AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1424990 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425168 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1499255 | Antiproliferative activity against human PF138 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1871768 | Inhibition of BLK (unknown origin) | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Review of the development of BTK inhibitors in overcoming the clinical limitations of ibrutinib. |
AID1560828 | Binding affinity to DNA-tagged recombinant ERBB4 (unknown origin) measured after 1 hr by biotinylated-ligand affinity bead-based qPCR analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1472026 | Growth inhibition of human OCI-LY10 cells at 0.003 uM after 3 days by AlamarBlue assay (Rvb = - 2 %) | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88 |
AID1720521 | Inhibition of His-tagged recombinant human His-tagged full length BTK expressed in baculovirus expression system using Tyr01 peptide as substrate preincubated for 1 hr by Z'lyte assay | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
| Discovery of quinoline-based irreversible BTK inhibitors. |
AID1499257 | Antiproliferative activity against human MOLM14 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1499264 | Antiproliferative activity against human NOMO1 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1397229 | Inhibition of recombinant human N-terminal GST-tagged JAK3 (781-end residues) expressed in baculovirus infected Sf9 cells using poly (4:1 Glu, Tyr) peptide as substrate after 60 mins by ADP-Glo assay | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
| Novel amino acid-substituted diphenylpyrimidine derivatives as potent BTK inhibitors against B cell lymphoma cell lines. |
AID1871760 | Inhibition of BTK (unknown origin) | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Review of the development of BTK inhibitors in overcoming the clinical limitations of ibrutinib. |
AID1412700 | Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay | 2018 | MedChemComm, Apr-01, Volume: 9, Issue:4
| Discovery and biological evaluation of N5-substituted 6,7-dioxo-6,7-dihydropteridine derivatives as potent Bruton's tyrosine kinase inhibitors. |
AID1424902 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1469915 | Effect on BTK transphosphorylation at PLCgamma2 Y759 in human Pfeiffer cells up to 1 uM measured after 4 hrs by chemiluminescent assay | | | |
AID1527026 | Growth inhibition of human OCI-LY10 cells at 10 nM incubated for 3 days by Alamar blue dye based fluorescence assay (Rvb = 3%) | | | |
AID1425012 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1673810 | In vivo protein occupancy at BTK in Wistar Han rat spleen assessed as BTK level in plasma at 10 mg/kg, po measured after 5 hrs | 2019 | ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
| Design of Potent and Selective Covalent Inhibitors of Bruton's Tyrosine Kinase Targeting an Inactive Conformation. |
AID1714844 | Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate incubate for 60 mins by LANCE assay | | | |
AID1822782 | Antitumor activity against human U-937 cells xenografted in Balb/c nude mouse assessed as supression in tumor growth at 25 mg/kg, po administered once daily 14 days | | | |
AID1638799 | Permeability of the compound assessed as drug flux at 500 uM after 16 hrs by PAMPA | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors. |
AID1738561 | Induction of cell cycle arrest in human Ramos cells assessed as S phase accumulation at 5 uM incubated for 24 hrs by PI staining based flow cytometry analysis (Rvb = 37.38 %) | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold. |
AID1718992 | Inhibition of EGFR (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 34 | Characterization of ibrutinib as a non-covalent inhibitor of SRC-family kinases. |
AID1623563 | Induction of apoptosis in human Ramos cells assessed as late apoptotic cells at 5 uM after 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometric analysis (Rvb = 0.98%) | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ. |
AID1324661 | Induction of apoptosis in human Ramos cells assessed as late apoptotic cells at 10 uM after 48 hrs by annexin V/FITC propidium iodide staining based flow cytometry relative to control | 2016 | ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
| Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing a |
AID1424992 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1894679 | Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Emerging small-molecule inhibitors of the Bruton's tyrosine kinase (BTK): Current development. |
AID1399807 | Inhibition of EGFR (unknown origin) at 1 uM relative to control | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
| Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit. |
AID1375562 | Toxicity in CB17 SCID nude mouse xenografted with human TMD8 cells assessed as change in body weight at 25 mg/kg, po qd administered for 13 consecutive days measured during compound dosing up to day 17 post dose | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
AID1425058 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1468807 | Inhibition of recombinant human cytoplasmic GST-tagged EGFR expressed in baculovirus at 1 uM by Z'-LYTE assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
| Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development. |
AID1718991 | Inhibition of BTK T333M mutant (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 34 | Characterization of ibrutinib as a non-covalent inhibitor of SRC-family kinases. |
AID1725086 | Cmax in Sprague-Dawley rat at 2 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery and Evaluation of Pyrazolo[3,4- |
AID1484559 | Cytotoxicity against human PBMC at 5 to 10 uM after 24 hrs by acridine orange/propidium iodide staining-based fluorescent microscopic analysis relative to control | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design and synthesis of sulfonamide-substituted diphenylpyrimidines (SFA-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B-cell lymphoblastic leukemia. |
AID1549552 | Antiproliferative activity against human Daudi cells | 2019 | European journal of medicinal chemistry, May-01, Volume: 169 | Design, synthesis and evaluation of novel 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as potent, selective and reversible Bruton's tyrosine kinase (BTK) inhibitors for the treatment of rheumatoid arthritis. |
AID1499239 | Antiproliferative activity against human A431 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1638810 | Efflux ratio of apparent permeability in MDCK2-MDR1 cells at 10 uM after 2 hrs by transwell membrane based assay | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors. |
AID1714871 | Inhibition of recombinant human LCK using Ulight-Poly GAT[EAY(1:1:1)]n as substrate incubate for 10 mins by LANCE assay | | | |
AID1718989 | Inhibition of SRC T338M/S345C double mutant (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 34 | Characterization of ibrutinib as a non-covalent inhibitor of SRC-family kinases. |
AID1871766 | Inhibition of ERBB2 (unknown origin) | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Review of the development of BTK inhibitors in overcoming the clinical limitations of ibrutinib. |
AID1397248 | Induction of apoptosis in human NAMALWA cells assessed as necrotic cells at 5 uM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 4.05%) | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
| Novel amino acid-substituted diphenylpyrimidine derivatives as potent BTK inhibitors against B cell lymphoma cell lines. |
AID1425145 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425034 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425163 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1418288 | Inhibition of CYP2C19 (unknown origin) | 2018 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
| Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk. |
AID1334890 | Cell cycle arrest in human Ramos cells assessed as accumulation at G2/M phase at 10 uM measured after 48 hrs by propidium iodide based flow cytometry (Rvb = 4.98 %) | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
| Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines. |
AID1425173 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425170 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1571251 | Antiproliferative activity against human Raji cells at 5 uM by MTT assay | | | |
AID1399797 | Inhibition of CYP2C9 (unknown origin) | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
| Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit. |
AID1738556 | Induction of apoptosis in human Ramos cells assessed as viable cells at 5 uM incubated for 24 hrs by annexin V-FITC and PI staining based flow cytometry analysis (Rvb = 93.8 %) | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold. |
AID1488736 | Inhibition of BMX (unknown origin) | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
| Discovery of (R)-5-(benzo[d][1,3]dioxol-5-yl)-7-((1-(vinylsulfonyl)pyrrolidin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (B6) as a potent Bmx inhibitor for the treatment of NSCLC. |
AID1375488 | Cmax in rat at 3 mg/kg, po | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
AID1869074 | Inhibition of His-tagged full-length recombinant wild-type human BTK (Ala2 to Ser659 residues) expressed in baculovirus infected insect cells incubated for 30 mins in presence of ATP by Microfluidic chip based mobility shift assay | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
| Medicinal Chemistry Strategies for the Development of Bruton's Tyrosine Kinase Inhibitors against Resistance. |
AID1425159 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1615376 | Selectivity ratio of IC50 for TEC (unknown origin) to IC50 for N-terminal His-tagged recombinant human BTK (393 to 659 residues) expressed in baculovirus infected Sf9 cells | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1714867 | Inhibition of FLT3 (unknown origin) | | | |
AID1425193 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424921 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1822762 | Inhibition of human BTK using poly-Glu-Tyr (4:1) as substrate incubated for 1 hr by ELISA | | | |
AID1375490 | AUC (0 to infinity) in rat at 3 mg/kg, po | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
AID1912478 | Inhibition of the Organic Cation Transporter 3 (OCT3, SLC22A3) as assessed by a phenotypic impedance-based assay detecting changes in cell morphology by MPP+ uptake in HEK-293 JumpIN-SLC22A3 cells (PubChem AID: 1745861) | 2022 | International journal of molecular sciences, Jan-21, Volume: 23, Issue:3
| MPP |
AID1425027 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425162 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1397230 | Inhibition of full length recombinant human N-terminal His-tagged BTK expressed in baculovirus infected Sf9 cells using poly (4:1 Glu, Tyr) peptide as substrate after 60 mins by ADP-Glo assay | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
| Novel amino acid-substituted diphenylpyrimidine derivatives as potent BTK inhibitors against B cell lymphoma cell lines. |
AID1458978 | Inhibition of recombinant human GST-tagged EGFR L858R/T790M double mutant expressed in baculovirus expression system preincubated for 30 mins followed by ATP and TK-substrate addition measured after 20 mins by HTRF assay | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1424923 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424896 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1718987 | Inhibition of SRC T338I mutant (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 34 | Characterization of ibrutinib as a non-covalent inhibitor of SRC-family kinases. |
AID1425070 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425044 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424925 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1334897 | Induction of apoptosis in human Ramos cells assessed as viable cells at 10 uM measured after 48 hrs by Annexin V-FITC/propidium iodide based flow cytometry relative to control | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
| Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines. |
AID1714777 | Cytotoxicity against human THP-1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | | | |
AID1375534 | Inhibition of recombinant human EPHA2 using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
AID1425113 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1571257 | Cell cycle arrest in human Ramos cells assessed as accumulation of cells at S phase at 5 uM after 48 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 71.08%) | | | |
AID1880571 | Invivo induction of BTK degradation in human OCILY10 cells xenografted in SCID mouse assessed as decrease in BTK level in tumor at 10 mg/kg, po administered once daily for 17 days by Western blot analysis | 2022 | Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
| Structural Feature Analyzation Strategies toward Discovery of Orally Bioavailable PROTACs of Bruton's Tyrosine Kinase for the Treatment of Lymphoma. |
AID1425029 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1375535 | Inhibition of recombinant human CSF1R using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
AID1499268 | Antiproliferative activity against human Rec1 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1424993 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424966 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1591631 | Inhibition of EGFR (unknown origin) | 2019 | Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
| Discovery and Biological evaluation of pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione derivatives as potent Bruton's tyrosine kinase inhibitors. |
AID1615387 | Inhibition of EGFR in human A431 cells assessed as reduction in EGFR phosphorylation at Tyr1068 residues preincubated for 1 hr followed by human EGF stimulation and measured after 10 mins by HTRF assay | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1425079 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1650552 | Antiproliferative activity against human JeKo1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | 2020 | Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
| Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors. |
AID1424960 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425046 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1470408 | Induction of apoptosis in human U2932 cells assessed as induction of caspase-3 cleavage at 10 uM after 48 hrs by immunoblot | | | |
AID1499249 | Antiproliferative activity against human U2932 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1375526 | Inhibition of recombinant human TEC using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
AID1574156 | Antiproliferative activity against human Mino cells after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
| Synthesis and biological evaluation of novel 1-substituted 3-(3-phenoxyprop-1-yn-1-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amines as potent Bruton's tyrosine kinase (BTK) inhibitors. |
AID1426158 | Cell cycle arrest in human Ramos cells assessed as accumulation at G2/M phase at 10 uM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 1.58%) | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines. |
AID1673811 | In vivo protein occupancy at BTK in Wistar Han rat spleen assessed as BTK level in plasma at 10 mg/kg, po measured after 0.5 hrs | 2019 | ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
| Design of Potent and Selective Covalent Inhibitors of Bruton's Tyrosine Kinase Targeting an Inactive Conformation. |
AID1714863 | Inhibition of FGR (unknown origin) | | | |
AID1468810 | Inhibition of recombinant human cytoplasmic full length His-tagged TEC expressed in baculovirus at 1 uM by Z'-LYTE assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
| Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development. |
AID1560831 | Selectivity ratio of Kd for DNA-tagged recombinant TEC (unknown origin) to Kd for DNA-tagged recombinant BTK (unknown origin) | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1375523 | Inhibition of recombinant human BLK using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
AID1425186 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424949 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1488738 | Inhibition of Her2 (unknown origin) | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
| Discovery of (R)-5-(benzo[d][1,3]dioxol-5-yl)-7-((1-(vinylsulfonyl)pyrrolidin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (B6) as a potent Bmx inhibitor for the treatment of NSCLC. |
AID1738559 | Induction of apoptosis in human Ramos cells assessed as necrotic cells at 5 uM incubated for 24 hrs by annexin V-FITC and PI staining based flow cytometry analysis (Rvb = 2.1 %) | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold. |
AID1424970 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1853204 | Inhibition of BTK (unknown origin) | 2022 | RSC medicinal chemistry, Dec-14, Volume: 13, Issue:12
| Advanced approaches of developing targeted covalent drugs. |
AID1870015 | Induction of apoptosis in human SU-DHL-6 cells assessed as early apoptotic cells at 1.5 uM incubated for 48 hrs by annexin V-FITC and PI staining based flow cytometry analysis (Rvb = 8.81 %) | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
| Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
AID1425128 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1334899 | Induction of apoptosis in human Ramos cells assessed as early apoptotic cells at 10 uM measured after 48 hrs by Annexin V-FITC/propidium iodide based flow cytometry relative to control | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
| Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines. |
AID1472000 | Growth inhibition of human OCI-LY10 cells at 0.0003 uM after 3 days by AlamarBlue assay (Rvb = - 2 %) | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88 |
AID1738562 | Induction of cell cycle arrest in human Ramos cells assessed as G2/M phase accumulation at 5 uM incubated for 24 hrs by PI staining based flow cytometry analysis (Rvb = 20.96 %) | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold. |
AID1425064 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425189 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1337175 | Inhibition of PF-06658607 binding to BTK in human Ramos cells after 1 hr by gel-based ABPP assay | 2017 | Nature reviews. Drug discovery, Jun, Volume: 16, Issue:6
| Non-kinase targets of protein kinase inhibitors. |
AID1391150 | Antiproliferative activity against human Raji cells after 48 hrs by CCK8-based assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Design, synthesis and biological evaluation of novel 3-substituted pyrazolopyrimidine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors. |
AID1549550 | Antiproliferative activity against human Ramos cells | 2019 | European journal of medicinal chemistry, May-01, Volume: 169 | Design, synthesis and evaluation of novel 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as potent, selective and reversible Bruton's tyrosine kinase (BTK) inhibitors for the treatment of rheumatoid arthritis. |
AID1425047 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1638807 | Protein binding in mouse plasma at 5 uM after 6 hrs by LC/MS analysis | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors. |
AID1560836 | Selectivity ratio of Kd for DNA-tagged recombinant JAK3 (unknown origin) to Kd for DNA-tagged recombinant BTK (unknown origin) | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1623566 | Cell cycle arrest in human Ramos cells assessed as accumulation at G0/G1 phase at 5 uM after 48 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 24.65%) | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ. |
AID1375486 | Volume of distribution at steady state in rat at 1 mg/kg, iv | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
AID1398713 | Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
| Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3Kδ. |
AID1499260 | Antiproliferative activity against human SKM1 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1424953 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425010 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1830230 | Inhibition of BTK C481S mutant (unknown origin) in presence of 1 mM ATP by microplate reader assay | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
| Discovery of AS-1763: A Potent, Selective, Noncovalent, and Orally Available Inhibitor of Bruton's Tyrosine Kinase. |
AID1571247 | Antiproliferative activity against human Ramos cells after 48 hrs by MTT assay | | | |
AID1725077 | Inhibition of human liver microsome CYP2D6 using dextromethorphan as substrate preincubated for 10 mins followed by substrate and NADPH addition and measured after 10 mins by LC-MS/MS analysis | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery and Evaluation of Pyrazolo[3,4- |
AID1418274 | Permeability across apical to basolateral side in human Caco2 cells | 2018 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
| Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk. |
AID1424920 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1571263 | Inhibition of BTK in human Ramos cells assessed as reduction in PLCgamma-2 phosphorylation at Try1217 residue at 100 to 3000 nM after 24 hrs by Western blot analysis | | | |
AID1499272 | Antiproliferative activity against primary CLL cells derived from p13 patient after 72 hrs by CellTiter-Glo assay | | | |
AID1499270 | Antiproliferative activity against human Z138 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1524883 | Antiproliferative activity against human Rec1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell-titer-Glo luminescent cell viability assay | 2019 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
| Discovery of novel pyrazole derivatives as potential anticancer agents in MCL. |
AID1424928 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425052 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425115 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1587021 | Inhibition of full-length human C-terminal His6-tagged BTK C481S mutant expressed in Sf9 insect cells using FAM-Srctide peptide as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr by TR-FRET Lanthascreen assay | 2019 | ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
| Aminopyrazole Carboxamide Bruton's Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning. |
AID1560796 | Inhibition of BTK in vitamin D3 differentiated human THP1 cells assessed as inhibition of FCgammaR-induced IL8 production measured after 24 hrs by HTRF assay | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1623565 | Induction of apoptosis in human Ramos cells assessed as viable cells at 5 uM after 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometric analysis (Rvb = 96.83%) | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ. |
AID1714778 | Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | | | |
AID1673839 | Inhibition of BTK in anti-IgM-stimulated human Ramos cells assessed as decrease in auto-phosphorylation at Tyr223 residue at 5 uM by immunoblot analysis | 2019 | ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
| Design of Potent and Selective Covalent Inhibitors of Bruton's Tyrosine Kinase Targeting an Inactive Conformation. |
AID1880541 | Antiproliferative activity against human MINO cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay | 2022 | Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
| Structural Feature Analyzation Strategies toward Discovery of Orally Bioavailable PROTACs of Bruton's Tyrosine Kinase for the Treatment of Lymphoma. |
AID1334877 | Inhibition of human recombinant full-length N-terminal His-tagged BTK expressed in baculovirus infected Sf9 insect cells measured after 60 mins by ADP-Glo kinase assay | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
| Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines. |
AID1375479 | Inhibition of recombinant human BTK using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
AID1424973 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1469889 | Inhibition of recombinant human N-terminal GST-tagged JAK3 (781 to end residues) expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 60 mins followed by substrate addition after 1 hr by ADP-Glo luminescen | | | |
AID1563062 | Cell cycle arrest in human Ramos cells assessed as accumulation at G2/M phase at 1 uM measured after 48 hrs by propidium iodide/RNase staining based flow cytometric analysis (Rvb = 5.98 %) | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines. |
AID1387235 | Inhibition of N-terminal DYKDDDDK tagged biotinylated unactivated human recombinant BTK using FITC-labeled Srctide peptide substrate by by mobility shift assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
| Design and Synthesis of Novel Amino-triazine Analogues as Selective Bruton's Tyrosine Kinase Inhibitors for Treatment of Rheumatoid Arthritis. |
AID1772877 | Antiproliferative activity against human OVCAR-4 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors. |
AID1738553 | Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold. |
AID1465441 | Inhibition of BTK (unknown origin) preincubated for 1 hr followed by ATP addition measured after 1 hr by immobilized metal ion affinity-based fluorescence polarization assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| In Silico Identification of a Novel Hinge-Binding Scaffold for Kinase Inhibitor Discovery. |
AID1876106 | Cytotoxicity against human DU-145 cells | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
AID1499238 | Antiproliferative activity against human HCT116 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1424995 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1549567 | Inhibition of human recombinant JAK3 using Ulight-CAGAGAIETDKEYYTVKD measured after 60 mins in the presence of ATP by LANCE method | 2019 | European journal of medicinal chemistry, May-01, Volume: 169 | Design, synthesis and evaluation of novel 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as potent, selective and reversible Bruton's tyrosine kinase (BTK) inhibitors for the treatment of rheumatoid arthritis. |
AID1869076 | Inhibition of BTK C481R mutant (unknown origin) expressed in baculovirus infected Trichoplusia ni pro cells incubated for 30 mins in presence of ATP by Microfluidic chip based mobility shift assay | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
| Medicinal Chemistry Strategies for the Development of Bruton's Tyrosine Kinase Inhibitors against Resistance. |
AID1524888 | Inhibition of human BTK assessed as remaining kinase activity at 1 uM using Cdc2 peptide KVEKIGEGTYGVVYK substrate and [gamma-33P]-ATP incubated for 40 mins by radiometric protein kinase assay | 2019 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
| Discovery of novel pyrazole derivatives as potential anticancer agents in MCL. |
AID1418277 | Protein binding in human plasma assessed as unbound fraction | 2018 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
| Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk. |
AID1425206 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425121 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1822772 | Antiproliferative activity against human U-937 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay | | | |
AID1424929 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1880137 | Inhibition of ITK (unknown origin) | 2022 | Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8
| The Ascension of Targeted Covalent Inhibitors. |
AID1425026 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1472025 | Growth inhibition of human OCI-LY10 cells at 0.001 uM after 3 days by AlamarBlue assay (Rvb = - 2 %) | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88 |
AID1870022 | Induction of apoptosis in human DOHH-2 cells assessed as viable cells at 1 uM incubated for 48 hrs by annexin V-FITC and PI staining based flow cytometry analysis (Rvb = 95.4 %) | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
| Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
AID1822765 | Selectivity ratio of IC50 for inhibition of human ITK using poly-Glu-Tyr (4:1) as substrate incubated for 1 hr by ELISA to IC50 for inhibition of human BTK using poly-Glu-Tyr (4:1) as substrate incubated for 1 hr by ELISA | | | |
AID1425153 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1475907 | Inhibition of 4EBP1 phosphorylation at Ser 65 residues in human Mino cells at 10 to 25 uM after 48 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
| Anchimerically Activated ProTides as Inhibitors of Cap-Dependent Translation and Inducers of Chemosensitization in Mantle Cell Lymphoma. |
AID1563070 | Cell cycle arrest in human Raji cells assessed as accumulation at S phase at 1 uM measured after 48 hrs by propidium iodide/RNase staining based flow cytometric analysis (Rvb = 33.18 %) | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines. |
AID1524884 | Antiproliferative activity against human JeKo1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell-titer-Glo luminescent cell viability assay | 2019 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
| Discovery of novel pyrazole derivatives as potential anticancer agents in MCL. |
AID1738557 | Induction of apoptosis in human Ramos cells assessed as early apoptotic cells at 5 uM incubated for 24 hrs by annexin V-FITC and PI staining based flow cytometry analysis (Rvb = 1.9 %) | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold. |
AID1638806 | Protein binding in human plasma at 5 uM after 6 hrs by LC/MS analysis | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors. |
AID1478517 | Cytotoxicity against human Ramos cells assessed as decrease in cell viability after 24 hrs by CellTiter-Glo assay | 2017 | Bioorganic & medicinal chemistry, 06-01, Volume: 25, Issue:11
| Identification of spirobisnaphthalene derivatives with anti-tumor activities from the endophytic fungus Rhytidhysteron rufulum AS21B. |
AID1772879 | Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors. |
AID1527024 | Growth inhibition of human OCI-LY10 cells at 2.1 nM incubated for 3 days by Alamar blue dye based fluorescence assay (Rvb = 3%) | | | |
AID1656243 | Inhibition of BTK in human whole blood cells assessed as apparent second order rate after 1 hr by ELISA | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
| Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK). |
AID1488734 | Antiproliferative activity against human HCC827 cells harboring EGFR Del19 mutant after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
| Discovery of (R)-5-(benzo[d][1,3]dioxol-5-yl)-7-((1-(vinylsulfonyl)pyrrolidin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (B6) as a potent Bmx inhibitor for the treatment of NSCLC. |
AID1894183 | Inhibition of BTK autophosphorylation in anti-IgG stimulated human DOHH-2 cells preincubated for 1 hr followed by compound washout and anti-IgG stimulation for 2 mins by chemiluminescence based Western blotting analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application. |
AID1571256 | Cell cycle arrest in human Ramos cells assessed as accumulation of cells at G0/G1 phase at 5 uM after 48 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 24.65%) | | | |
AID1549564 | Inhibition of human recombinant EGFR using Ulight-CAGAGAIETDKEYYTVKD measured after 15 mins in the presence of ATP by LANCE method | 2019 | European journal of medicinal chemistry, May-01, Volume: 169 | Design, synthesis and evaluation of novel 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as potent, selective and reversible Bruton's tyrosine kinase (BTK) inhibitors for the treatment of rheumatoid arthritis. |
AID1425116 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1725072 | Cmax in BALB/c mouse 2 mg/kg, po measured upto 24 hrs by LC-MS/MS analysis | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery and Evaluation of Pyrazolo[3,4- |
AID1412711 | Inhibition of human ITK using using myelin basic protein as substrate measured after 1 hr in presence of [gamma-33P]ATP | 2018 | MedChemComm, Apr-01, Volume: 9, Issue:4
| Discovery and biological evaluation of N5-substituted 6,7-dioxo-6,7-dihydropteridine derivatives as potent Bruton's tyrosine kinase inhibitors. |
AID1692288 | Inhibition of human platelet adhesion to immobilised CRP-XL at 1 umol/L preincubated for 4 mins followed by CRP-XL addition and measured after 45 mins relative to control | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Progress toward a Glycoprotein VI Modulator for the Treatment of Thrombosis. |
AID631100 | Inhibition of human full-length BTK expressed in Sf9 cells using FAM-Srctide peptide as substrate after 60 mins by TR-FRET Assay | 2011 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
| Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis. |
AID1878118 | Binding affinity to EGFR (unknown origin) assessed as dissociation constant by KINOMEscan analysis | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors. |
AID1425081 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425043 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1615380 | Selectivity ratio of IC50 for human BMX to IC50 for N-terminal His-tagged recombinant human BTK (393 to 659 residues) expressed in baculovirus infected Sf9 cells | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1714854 | Inhibition of RSK1 (unknown origin) | | | |
AID1615346 | Selectivity ratio of IC50 for EGFR (unknown origin) to IC50 for N-terminal His-tagged recombinant human BTK (393 to 659 residues) expressed in baculovirus infected Sf9 cells | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1851531 | Antiproliferative activity against human Raji cells incubated for 72 hrs by CellTiter-Glo assay | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Design, synthesis, and biological evaluation of pyrrolopyrimidine derivatives as novel Bruton's tyrosine kinase (BTK) inhibitors. |
AID1714872 | Inhibition of recombinant human LYN using biotinyl-beta Abeta-Abeta AKVEKIGEGTYGVVYK as substrate incubate for 120 mins by LANCE assay | | | |
AID1880547 | Inhibition of BTK (unknown origin) | 2022 | Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
| Structural Feature Analyzation Strategies toward Discovery of Orally Bioavailable PROTACs of Bruton's Tyrosine Kinase for the Treatment of Lymphoma. |
AID1781997 | Inhibition of full-length N-terminal GST-tagged BMX (1 to 675 residues) (unknown origin) expressed in Sf21 insect cells using NH2-ETVYSEVRK-biotin as substrate preincubated for 1 hr followed by ATP addition and measured after 2 hrs by ELISA | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
| Discovery of 1-Amino-1 |
AID1499244 | Antiproliferative activity against human HeLa cells after 72 hrs by CellTiter-Glo assay | | | |
AID1673813 | In vivo protein occupancy at BTK in Wistar Han rat spleen at 10 mg/kg, po measured after 5 hrs relative to control | 2019 | ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
| Design of Potent and Selective Covalent Inhibitors of Bruton's Tyrosine Kinase Targeting an Inactive Conformation. |
AID1412699 | Inhibition of recombinant human full-length N-terminal His6-tagged BTK expressed in baculovirus infected Sf21insect cells using poly (4:1 Glu, Tyr) as substrate measured after 1 hr by ELISA | 2018 | MedChemComm, Apr-01, Volume: 9, Issue:4
| Discovery and biological evaluation of N5-substituted 6,7-dioxo-6,7-dihydropteridine derivatives as potent Bruton's tyrosine kinase inhibitors. |
AID1424989 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1615446 | Oral bioavailability in human in fasting state at 560 mg administered daily | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1426139 | Inhibition of N-terminal His-tagged full length human recombinant BTK expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) peptide substrate incubated for 60 mins by ADP-Glo luminescence assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines. |
AID1714775 | Aqueous solubility of compound at 1 mg | | | |
AID1615377 | Selectivity ratio of IC50 for JAK3 (unknown origin) to IC50 for N-terminal His-tagged recombinant human BTK (393 to 659 residues) expressed in baculovirus infected Sf9 cells | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1425134 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1615390 | Selectivity ratio of IC50 for EGFR in human A431 cells to IC50 for BTK in human Ramos cells | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1524891 | Hepatic clearance in human liver microsomes further incubated of 5 to 60 mins in presence of NADPH regenerating system by LC/MS analysis | 2019 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
| Discovery of novel pyrazole derivatives as potential anticancer agents in MCL. |
AID1424910 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425126 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1591652 | Antiproliferative activity against human resistant Jeko cells assessed as reduction in viability after 72 hrs by CellTiter-Glo luminescent assay | 2019 | Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
| Design, synthesis and biological evaluation of novel 2,3-indolinedione derivatives against mantle cell lymphoma. |
AID1424962 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1481310 | Inhibition of Tel-fused EGFR T790M mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1424996 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1304227 | Inhibition of BTK (unknown origin) assessed as reduction in phosphorylation of coumarin and fluorescein-labeled FRET peptide substrate at 10 uM incubated for 1 hr by Z-Lyte assay relative to control | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Structure-based discovery of novel 4,5,6-trisubstituted pyrimidines as potent covalent Bruton's tyrosine kinase inhibitors. |
AID1375487 | Half life in rat at 1 mg/kg, iv | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
AID1872694 | Antitumor activity against human DOHH-2 cells xenografted in CB17/SCID mouse assessed as reduction in tumor growth at 30 mg/kg, po administered once daily in combination with idelalisib at 50 mg/kg for 30 days and measured twice a week relative to control | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Recent development of BTK-based dual inhibitors in the treatment of cancers. |
AID1425172 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1720530 | Inhibition of EGFR phosphorylation in human A431 cells | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
| Discovery of quinoline-based irreversible BTK inhibitors. |
AID1720523 | Inhibition of His-tagged recombinant full length human His-tagged BMX cytoplasmic domain expressed in baculovirus expression system using tyrosine-1 peptide as substrate preincubated for 1 hr in presence of ATP by Z'-LYTE assay | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
| Discovery of quinoline-based irreversible BTK inhibitors. |
AID1424898 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425137 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1417604 | Volume of distribution at steady state in mouse at 0.2 mg/kg, iv administered as single dose | 2018 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20
| Optimization of the efflux ratio and permeability of covalent irreversible BTK inhibitors. |
AID1425105 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1880561 | Antitumor activity against human OCILY10 cells xenografted in SCID mouse assessed as tumor growth inhibition at 10 mg/kg, po qd measured after 17 days relative to control | 2022 | Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
| Structural Feature Analyzation Strategies toward Discovery of Orally Bioavailable PROTACs of Bruton's Tyrosine Kinase for the Treatment of Lymphoma. |
AID1673828 | Inhibition of BTK in vitamin D3 differentiated human THP1 cells assessed as inhibition of FCgammaR-induced IL8 production measured after 24 hrs by immunoblot analysis | 2019 | ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
| Design of Potent and Selective Covalent Inhibitors of Bruton's Tyrosine Kinase Targeting an Inactive Conformation. |
AID1469900 | Growth inhibition of human OCI-AML3 cells | | | |
AID1417608 | Inhibition of BTK in human WBC | 2018 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20
| Optimization of the efflux ratio and permeability of covalent irreversible BTK inhibitors. |
AID1425090 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1714869 | Inhibition of recombinant human YES using biotinyl-beta Abeta-Abeta AYQAEENTYDEYEN as substrate incubate for 30 mins by LANCE assay | | | |
AID1499266 | Antiproliferative activity against human OCI-AML2 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1571262 | Inhibition of BTK phosphorylation at Tyr223 residue in human Ramos cells at 100 to 3000 nM after 24 hrs by Western blot analysis | | | |
AID1418273 | Inhibition of BTK in goat anti-human IgM F(ab')2-stimulated human PBMC assessed as suppression of BCR-induced CD69 expression on B cells pretreated for 1 hr followed by blood stimulation measured after overnight incubation by flow cytometry | 2018 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
| Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk. |
AID1587600 | Antiproliferative activity against human Mino cells measured after 72 hrs by calcein AM dye-based fluorescence assay | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
| 3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models. |
AID1650556 | Metabolic stability in human liver microsomes assessed as compound remaining at 0.2 uM incubated for 60 mins by UPLC-MS/MS analysis | 2020 | Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
| Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors. |
AID1418280 | Half life in mouse at 0.5 mg/kg, po | 2018 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
| Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk. |
AID1553406 | Inhibition of human recombinant full length BTK expressed in baculovirus in Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate incubated for 1 hr by ADP-Glo assay | 2019 | Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
| Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors. |
AID1424994 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1399794 | Inhibition of CYP2C8 (unknown origin) | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
| Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit. |
AID1650543 | Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay | 2020 | Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
| Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors. |
AID1387234 | Inhibition of N-terminal DYKDDDDK tagged biotinylated activated human recombinant BTK using FITC-labeled Srctide peptide substrate by mobility shift assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
| Design and Synthesis of Novel Amino-triazine Analogues as Selective Bruton's Tyrosine Kinase Inhibitors for Treatment of Rheumatoid Arthritis. |
AID1425037 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1656237 | Metabolic stability in human liver microsomes assessed as parent compound remaining after 10 mins | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
| Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK). |
AID1375532 | Inhibition of recombinant human BMX using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
AID1472027 | Growth inhibition of human OCI-LY10 cells at 0.017 uM after 3 days by AlamarBlue assay (Rvb = - 2 %) | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88 |
AID1425198 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1781998 | Inhibition of full-length N-terminal GST-tagged ITK (2 to 620 residues) (unknown origin) expressed in Sf21 insect cells using NH2-ETVYSEVRK-biotin as substrate preincubated for 1 hr followed by ATP addition and measured after 2 hrs by ELISA | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
| Discovery of 1-Amino-1 |
AID1465438 | Inhibition of human BTK using KVEKIGEGTYGVVYK as substrate preincubated for 20 mins followed by [gamma-33P]-ATP addition by filter binding method | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| In Silico Identification of a Novel Hinge-Binding Scaffold for Kinase Inhibitor Discovery. |
AID1822807 | Inhibition of EGFR phosphorylation in human A549 cells at 100 nM incubated for 4 hrs by Western blot analysis | | | |
AID1851524 | Antiproliferative activity against human REC1 cells incubated for 72 hrs by CellTiter-Glo assay | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Design, synthesis, and biological evaluation of pyrrolopyrimidine derivatives as novel Bruton's tyrosine kinase (BTK) inhibitors. |
AID1738555 | Inhibition of BTK (unknown origin) by ADP-Glo assay | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold. |
AID1484555 | Antiproliferative activity against human Raji cells over expressing BTK after 48 hrs by CCK-8 assay | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design and synthesis of sulfonamide-substituted diphenylpyrimidines (SFA-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B-cell lymphoblastic leukemia. |
AID1499247 | Antiproliferative activity against human C4-2 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1563021 | Antiproliferative activity against human Ramos cells at 40 uM measured after 72 hrs by CCK-8 assay relative to control | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines. |
AID1499252 | Antiproliferative activity against human NAMALWA cells after 72 hrs by CellTiter-Glo assay | | | |
AID1472052 | Antitumor activity against human OCI-LY10 cells xenografted in SCID CB.17 mouse assessed as tumor growth inhibition at 12 mg/kg, po qd after 34 days post inoculation measured on day 51 relative to control | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88 |
AID1878124 | Selectivity index, ratio of Kd for EGFR (unknown origin) to Kd for BTK (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors. |
AID1650545 | Inhibition of recombinant human N-terminal GST-tagged TYK2 (871 to 1187 residues) expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay | 2020 | Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
| Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors. |
AID1425086 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425191 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1538544 | Inhibition of MKK7 beta1 S273D/T275D double mutant (unknown origin) assessed as residual activity at 50 uM using JNK1 K55M mutant as substrate by ADP-Glo assay relative to control | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| Characterization of Covalent Pyrazolopyrimidine-MKK7 Complexes and a Report on a Unique DFG-in/Leu-in Conformation of Mitogen-Activated Protein Kinase Kinase 7 (MKK7). |
AID1468764 | Inhibition of recombinant human cytoplasmic His-tagged ERBB2 expressed in baculovirus at 1 uM by Z'-LYTE assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
| Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development. |
AID1399800 | Volume of distribution at steady state in rat at 0.5 mg/kg, po | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
| Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit. |
AID1469901 | Growth inhibition of human Pfeiffer cells | | | |
AID1399791 | Fraction unbound in mouse plasma | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
| Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit. |
AID1615343 | Inhibition of BTK in human Ramos cells assessed as reduction in BTK phosphorylation at Tyr223 residue preincubated for 1 hr followed by pervanadate or Na3VO4 stimulation for 20 mins by HTRF assay | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1401339 | Inhibition of BTK phosphorylation in human NAMALWA cells at 10 uM after 48 hrs by immunoblot analysis | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma. |
AID1591651 | Antiproliferative activity against human Z138 cells assessed as reduction in viability after 72 hrs by CellTiter-Glo luminescent assay | 2019 | Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
| Design, synthesis and biological evaluation of novel 2,3-indolinedione derivatives against mantle cell lymphoma. |
AID1465440 | Selectivity ratio of IC50 for human TEC to IC50 for human BTK | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| In Silico Identification of a Novel Hinge-Binding Scaffold for Kinase Inhibitor Discovery. |
AID1425007 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1401309 | Antiproliferative activity against human Ramos cells after 72 hrs by CCK-8 assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma. |
AID1650550 | Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | 2020 | Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
| Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors. |
AID1424915 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1468826 | Inhibition of BTK in human whole blood derived-basophils assessed as suppression of IgE mediated-FcepsilonR ligation-stimulated CD63 expression | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
| Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development. |
AID1469906 | Cytotoxicity against PBMC (unknwon origin) | | | |
AID1809419 | Inhibition of Btk (unknown origin) assessed as ratio of Kinact/Ki | 2021 | Journal of medicinal chemistry, 09-09, Volume: 64, Issue:17
| Discovery of the Bruton's Tyrosine Kinase Inhibitor Clinical Candidate TAK-020 ( |
AID1425094 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1725081 | Inhibition of human liver microsome CYP3A4 using midazolam as substrate preincubated for 10 mins followed by substrate and NADPH addition and measured after 10 mins by LC-MS/MS analysis | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery and Evaluation of Pyrazolo[3,4- |
AID1714776 | Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | | | |
AID1399783 | Permeability from apical to basolateral side in human Caco2 cells | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
| Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit. |
AID1878103 | Selectivity index, ratio of Kd for BLK (unknown origin) to Kd for BTK (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors. |
AID1488733 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
| Discovery of (R)-5-(benzo[d][1,3]dioxol-5-yl)-7-((1-(vinylsulfonyl)pyrrolidin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (B6) as a potent Bmx inhibitor for the treatment of NSCLC. |
AID1425071 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1481311 | Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1424987 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425077 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1484560 | Induction of apoptosis in human Ramos cells assessed as viable cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric analysis relative to control | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design and synthesis of sulfonamide-substituted diphenylpyrimidines (SFA-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B-cell lymphoblastic leukemia. |
AID1830234 | Antiproliferative activity against human OCILY10 cells harboring BTK C481S mutant knockout gene assessed as reduction in cell viability after 96 hrs | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
| Discovery of AS-1763: A Potent, Selective, Noncovalent, and Orally Available Inhibitor of Bruton's Tyrosine Kinase. |
AID1155538 | Toxicity in CB17 SCID mouse xenografted with human DOHH2 cells assessed as body weight fluctuations at 10 mg/kg, iv qd administered for 14 days measured over 14 days of compound treatment | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity. |
AID1615364 | Inhibition of ITK (unknown origin) preincubated for 1 hr followed by Biotin-AVLESEEELYSSARQ-NH2 substrate addition in presence of ATP and measured after 1 hr by TR-FRET assay | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1469890 | Inhibition of recombinant human N-terminal GST-tagged wild-type EGFR (695 to end residues) expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 60 mins followed by substrate addition after 1 hr by ADP-Glo | | | |
AID1472051 | Growth inhibition of human SUDHL2 cells at 0.017 uM after 3 days by AlamarBlue assay (Rvb = - 1 %) | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88 |
AID1425167 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425038 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425207 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1418282 | AUC in mouse at 0.5 mg/kg, po | 2018 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
| Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk. |
AID1878125 | Selectivity index, ratio of Kd for ERBB2 (unknown origin) to Kd for BTK (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors. |
AID1772885 | Antiproliferative activity against human U-251 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors. |
AID671744 | Inhibition of RET | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies. |
AID1781996 | Inhibition of full-length N-terminal GST tagged BTK (2 to 659 residues) (unknown origin) expressed in Sf21 insect cells using NH2-ETVYSEVRK-biotin as substrate preincubated for 1 hr followed by ATP addition and measured after 2 hrs by ELISA | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
| Discovery of 1-Amino-1 |
AID1563020 | Inhibition of human recombinant full length N-terminal His tagged BTK expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate measured after 60 mins in presence of ATP by ADP-Glo kinase assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines. |
AID1880542 | Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay | 2022 | Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
| Structural Feature Analyzation Strategies toward Discovery of Orally Bioavailable PROTACs of Bruton's Tyrosine Kinase for the Treatment of Lymphoma. |
AID1398711 | Antiproliferative activity against human Raji cells after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
| Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3Kδ. |
AID1424890 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1673827 | Inhibition of EGF-induced EGFR phosphorylation in human A431 cells preincubated for 24 hrs followed by EGF stimulation and measured after 10 mins by HTRF based immunoassay | 2019 | ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
| Design of Potent and Selective Covalent Inhibitors of Bruton's Tyrosine Kinase Targeting an Inactive Conformation. |
AID1587597 | Inhibition of His-tagged CDK2/Cyclin-E1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
| 3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models. |
AID1718986 | Inhibition of SRC S345C mutant (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 34 | Characterization of ibrutinib as a non-covalent inhibitor of SRC-family kinases. |
AID1424945 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424958 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425132 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1714864 | Inhibition of FRK (unknown origin) | | | |
AID1425101 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1391149 | Antiproliferative activity against human Ramos cells after 48 hrs by CCK8-based assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Design, synthesis and biological evaluation of novel 3-substituted pyrazolopyrimidine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors. |
AID1425017 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1476271 | Antiproliferative activity against human MV4-11 cells after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
AID1426146 | Induction of apoptosis in human Ramos cells assessed as late apoptotic cells at 10 uM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 3%) | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines. |
AID1425171 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425019 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424983 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1399799 | Clearance in rat at 0.5 mg/kg, po | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
| Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit. |
AID1499235 | Inhibition of TEL-fused JAK1 (unknown origin) expressed in mouse BA/F3 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1870003 | Induction of cell cycle arrest in human SU-DHL-6 cells assessed as accumulation of cells at G2/M phase at 0.5 uM incubated for 24 hrs by PI staining based FACScan flow cytometry analysis (Rvb = 20.21 %) | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
| Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
AID1587599 | Antiproliferative activity against human OCI-Ly2 cells measured after 72 hrs by calcein AM dye-based fluorescence assay | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
| 3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models. |
AID1424934 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1401317 | Induction of apoptosis in human Ramos cells assessed as necrotic cells at 10 uM after 72 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.7%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma. |
AID1309831 | Cytotoxicity against human A2780 cells assessed as cell growth inhibition after 3 days by presto blue dye based plate reader method | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Isatin Derived Spirocyclic Analogues with α-Methylene-γ-butyrolactone as Anticancer Agents: A Structure-Activity Relationship Study. |
AID1425092 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1615381 | Selectivity ratio of IC50 for human BRK to IC50 for N-terminal His-tagged recombinant human BTK (393 to 659 residues) expressed in baculovirus infected Sf9 cells | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1424937 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1468806 | Inhibition of recombinant human catalytic GST-tagged JAK3 expressed in baculovirus at 1 uM by Z'-LYTE assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
| Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development. |
AID1425065 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1499240 | Antiproliferative activity against human NCI-H460 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1870025 | Induction of apoptosis in human DOHH-2 cells assessed as necrotic cells at 1 uM incubated for 48 hrs by annexin V-FITC and PI staining based flow cytometry analysis (Rvb =0.29 %) | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
| Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
AID1425178 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1870024 | Induction of apoptosis in human DOHH-2 cells assessed as late apoptotic cells at 1 uM incubated for 48 hrs by annexin V-FITC and PI staining based flow cytometry analysis (Rvb = 2.20 %) | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
| Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
AID1615384 | Selectivity ratio of IC50 for human FRK to IC50 for N-terminal His-tagged recombinant human BTK (393 to 659 residues) expressed in baculovirus infected Sf9 cells | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1725078 | Inhibition of human liver microsome CYP2C19 using S-mephenytoin as substrate preincubated for 10 mins followed by substrate and NADPH addition and measured after 10 mins by LC-MS/MS analysis | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery and Evaluation of Pyrazolo[3,4- |
AID1720527 | Inhibition of recombinant human N-terminal GST-tagged ERBB4 catalytic domain (708 to 993 residues) expressed in baculovirus expression system using tyrosine-1 peptide as substrate preincubated for 1 hr in presence of ATP by Z'-LYTE assay | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
| Discovery of quinoline-based irreversible BTK inhibitors. |
AID1880523 | Induction of BTK degradation in human MINO cells at 1000 nM incubated for 24 hrs by Western blot analysis | 2022 | Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
| Structural Feature Analyzation Strategies toward Discovery of Orally Bioavailable PROTACs of Bruton's Tyrosine Kinase for the Treatment of Lymphoma. |
AID1424950 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1772880 | Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors. |
AID1851527 | Antiproliferative activity against human SU-DHL-4 cells incubated for 72 hrs by CellTiter-Glo assay | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Design, synthesis, and biological evaluation of pyrrolopyrimidine derivatives as novel Bruton's tyrosine kinase (BTK) inhibitors. |
AID1830229 | Inhibition of wild type BTK (unknown origin) in presence of 1 mM ATP by microplate reader assay | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
| Discovery of AS-1763: A Potent, Selective, Noncovalent, and Orally Available Inhibitor of Bruton's Tyrosine Kinase. |
AID1560881 | Covalent binding affinity to BTK in human blood assessed as reduction in biotinylated-probe binding at 300 nM measured up to 100 mins by immunoassay relative to control | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1527023 | Growth inhibition of human OCI-LY10 cells at 0.3 nM incubated for 3 days by Alamar blue dye based fluorescence assay (Rvb = 3%) | | | |
AID1673823 | Immunostimulatory activity in ovalbumin-immunized C57Bl6 mouse assessed as reduction in skin swelling at 30 mg/kg, po administered 2 h prior to OVA immunization and measured after 5 hrs by caliper method relative to control | 2019 | ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
| Design of Potent and Selective Covalent Inhibitors of Bruton's Tyrosine Kinase Targeting an Inactive Conformation. |
AID1878126 | Selectivity index, ratio of Kd for ERBB4 (unknown origin) to Kd for BTK (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors. |
AID1871769 | Inhibition of JAK3 (unknown origin) | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Review of the development of BTK inhibitors in overcoming the clinical limitations of ibrutinib. |
AID1615367 | Inhibition of human BLK using poly[Glu:Tyr] (4:1) as substrate preincubated for 60 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by filter binding method | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1851504 | Inhibition of BTK (unknown origin) measured by ADP-Glo assay | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Design, synthesis, and biological evaluation of pyrrolopyrimidine derivatives as novel Bruton's tyrosine kinase (BTK) inhibitors. |
AID1425035 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1468772 | Inhibition of BTK in human whole blood-derived CD19+ B cells assessed as suppression of anti-IgM stimulated-CD69 expression preincubated for 1 hr followed by IgM stimulation for 18 hrs by FACS analysis | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
| Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development. |
AID1741721 | Inhibition of BTK (unknown origin) using poly(Glu, Tyr) 4:1 as substrate incubated in presence of [gamma33P]ATP by image analyser | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Scaffold hopping of the SYK inhibitor entospletinib leads to broader targeting of the BCR signalosome. |
AID1424977 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1563024 | Antiproliferative activity against human Raji cells measured after 72 hrs by CCK-8 assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines. |
AID1558403 | Inhibition of BTK (unknown origin) after 60 mins by FRET assay | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
| The Exploration of Chirality for Improved Druggability within the Human Kinome. |
AID1851505 | Antiproliferative activity against human TMD8 cells incubated for 72 hrs by CellTiter-Glo assay | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Design, synthesis, and biological evaluation of pyrrolopyrimidine derivatives as novel Bruton's tyrosine kinase (BTK) inhibitors. |
AID1499234 | Inhibition of TEL-fused BMX (unknown origin) expressed in mouse BA/F3 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1309836 | Cytotoxicity against human SW480 cells assessed as cell growth inhibition after 3 days by presto blue dye based plate reader method | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Isatin Derived Spirocyclic Analogues with α-Methylene-γ-butyrolactone as Anticancer Agents: A Structure-Activity Relationship Study. |
AID1560835 | Selectivity ratio of Kd for DNA-tagged recombinant ERBB4 (unknown origin) to Kd for DNA-tagged recombinant BTK (unknown origin) | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1499273 | Antiproliferative activity against primary CLL cells derived from p14 patient after 72 hrs by CellTiter-Glo assay | | | |
AID1650541 | Inhibition of recombinant human His-tagged full length BTK expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay | 2020 | Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
| Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors. |
AID1587025 | Reversible inhibition of human EGFR cytoplasmic domain expressed in baculovirus expression system assessed as ratio of Kinact to Ki using FITC-C6-KKAEEEEYFELVAKK-NH2 as substrate after 120 mins by caliper method | 2019 | ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
| Aminopyrazole Carboxamide Bruton's Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning. |
AID671742 | Inhibition of BLK | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies. |
AID1654023 | Inhibition of recombinant human N-terminal GST-tagged JAK3 (781 to end residues) expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins in presence of ATP by ADP-Glo kinase assay | 2020 | Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
| Synthesis and biological activity of thieno[3,2-d]pyrimidines as potent JAK3 inhibitors for the treatment of idiopathic pulmonary fibrosis. |
AID1851529 | Antiproliferative activity against human SU-DHL-6 cells incubated for 72 hrs by CellTiter-Glo assay | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Design, synthesis, and biological evaluation of pyrrolopyrimidine derivatives as novel Bruton's tyrosine kinase (BTK) inhibitors. |
AID1425048 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1476270 | Antiproliferative activity against mouse BAF3 cells harboring FLT3-ITD-F691L mutation after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
AID1425156 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1309834 | Cytotoxicity against human HeLa cells expressing GFP assessed as cell growth inhibition after 3 days by presto blue dye based plate reader method | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Isatin Derived Spirocyclic Analogues with α-Methylene-γ-butyrolactone as Anticancer Agents: A Structure-Activity Relationship Study. |
AID1894184 | Inhibition of PLCgamma phosphorylation in anti-IgG stimulated human DOHH-2 cells preincubated for 1 hr followed by compound washout and anti-IgG stimulation for 2 mins by chemiluminescence based Western blotting analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application. |
AID1425072 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424968 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425088 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424984 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1399795 | Inhibition of CYP2B6 (unknown origin) | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
| Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit. |
AID1822764 | Inhibition of GST-tagged human EGFR (668 to 1210 residues) expressed in baculovirus expression system using poly-Glu-Tyr (4:1) as substrate incubated for 1 hrs by ELISA | | | |
AID1822770 | Selectivity ratio of IC50 for inhibition of ITK phosphorylation in human Jurkat cells to IC50 for inhibition of BTK phosphorylation in human U-937 cells | | | |
AID1417597 | Permeability of the compound across apical to basolateral side in human Caco2 cells | 2018 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20
| Optimization of the efflux ratio and permeability of covalent irreversible BTK inhibitors. |
AID1425062 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1399796 | Inhibition of CYP2C19 (unknown origin) | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
| Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit. |
AID1822766 | Selectivity ratio of IC50 for human EGFR expressed in baculovirus expression system using poly-Glu-Tyr (4:1) as substrate incubated for 1 hr by ELISA to IC50 for inhibition of human BTK using poly-Glu-Tyr (4:1) as substrate incubated for 1 hr by ELISA | | | |
AID1714774 | Inhibition of BTK (unknown origin) by caliper mobility shift assay | | | |
AID1469902 | Growth inhibition of human U937 cells | | | |
AID1418275 | Efflux ratio of permeability in human Caco2 cells | 2018 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
| Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk. |
AID1720525 | Inhibition of recombinant human N-terminal GST-tagged TXK (260 to 527 residues) expressed in baculovirus expression system using tyrosine-6 peptide as substrate preincubated for 1 hr in presence of ATP by Z'-LYTE assay | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
| Discovery of quinoline-based irreversible BTK inhibitors. |
AID1499265 | Antiproliferative activity against human OCI-AML3 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1425139 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425185 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1549553 | Inhibition of BTK (unknown origin) in the presence of ATP by caliper mobility shift assay | 2019 | European journal of medicinal chemistry, May-01, Volume: 169 | Design, synthesis and evaluation of novel 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as potent, selective and reversible Bruton's tyrosine kinase (BTK) inhibitors for the treatment of rheumatoid arthritis. |
AID1615389 | Inhibition of TEC phosphorylation in HEK293 cells peincubated for 3 hrs followed by pervanadate stimulation and measured after 20 mins by MSD assay | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1399793 | Binding affinity to human ERG | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
| Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit. |
AID1488732 | Antiproliferative activity against human A549 cells harboring wild type EGFR after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
| Discovery of (R)-5-(benzo[d][1,3]dioxol-5-yl)-7-((1-(vinylsulfonyl)pyrrolidin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (B6) as a potent Bmx inhibitor for the treatment of NSCLC. |
AID1459010 | Antiproliferative activity against human A549 cells harboring KRAS-G12S mutant at 30 uM incubated for 96 hrs measured on day 5 by CellTiterGlo assay | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1426142 | Antiproliferative activity against human Raji cells after 48 hrs by CCK-8 assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines. |
AID1499248 | Antiproliferative activity against human SUDHL2 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1623553 | Antiproliferative activity against human Ramos cells after 48 hrs by CCK8 assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ. |
AID1623567 | Cell cycle arrest in human Ramos cells assessed as accumulation at S phase at 5 uM after 48 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 71.08%) | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ. |
AID1425011 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1499269 | Antiproliferative activity against human JVM2 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1587598 | Antiproliferative activity against human HT cells measured after 72 hrs by calcein AM dye-based fluorescence assay | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
| 3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models. |
AID1563061 | Cell cycle arrest in human Ramos cells assessed as accumulation at S phase at 1 uM measured after 48 hrs by propidium iodide/RNase staining based flow cytometric analysis (Rvb = 56.35 %) | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines. |
AID1425146 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1830233 | Inhibition of BTK in human whole blood assessed as activation of anti-IgM-induced CD69 expression by flow cytometry analysis | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
| Discovery of AS-1763: A Potent, Selective, Noncovalent, and Orally Available Inhibitor of Bruton's Tyrosine Kinase. |
AID1267793 | Cytotoxicity against mouse BAF3 cells assessed as cell proliferation after 72 hrs by CelltiterGlo assay | 2015 | Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
| Discovery of (R)-1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)-2-(dimethylamino)ethanone (CHMFL-FLT3-122) as a Potent and Orally Available FLT3 Kinase Inhibitor for FLT3-ITD Positive Acute Myeloid Leukemia. |
AID1650931 | Inhibition of BTK C481S mutant (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 30, Issue:3
| Design, synthesis and biological evaluation of Proteolysis Targeting Chimeras (PROTACs) as a BTK degraders with improved pharmacokinetic properties. |
AID1527029 | Growth inhibition of human OCI-LY19 cells at 2.1 nM incubated for 3 days by Alamar blue dye based fluorescence assay (Rvb = 3%) | | | |
AID1527025 | Growth inhibition of human OCI-LY10 cells at 4.2 nM incubated for 3 days by Alamar blue dye based fluorescence assay (Rvb = 3%) | | | |
AID1524890 | Intrinsic clearance in human liver microsomes further incubated of 5 to 60 mins in presence of NADPH regenerating system by LC/MS analysis | 2019 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
| Discovery of novel pyrazole derivatives as potential anticancer agents in MCL. |
AID1524889 | Half life in human liver microsomes further incubated of 5 to 60 mins in presence of NADPH regenerating system by LC/MS analysis | 2019 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
| Discovery of novel pyrazole derivatives as potential anticancer agents in MCL. |
AID1426144 | Induction of apoptosis in human Ramos cells assessed as viable cells at 10 uM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 94.3%) | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines. |
AID1425118 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1241391 | Inhibition of human recombinant BTK incubated for 5 mins by HTRF kinase assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
| Discovery of thieno[3,2-c]pyridin-4-amines as novel Bruton's tyrosine kinase (BTK) inhibitors. |
AID1425160 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424936 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1591625 | Inhibition of BTK (unknown origin) by ELISA | 2019 | Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
| Discovery and Biological evaluation of pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione derivatives as potent Bruton's tyrosine kinase inhibitors. |
AID1399798 | Inhibition of CYP3A4 (unknown origin) | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
| Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit. |
AID1720526 | Inhibition of His-tagged human recombinant ERBB2 (676 to 1255 residues) expressed in baculovirus expression system using Tyr 06 as substrate preincubated for 1 hr in presence of ATP by Z'-LYTE assay | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
| Discovery of quinoline-based irreversible BTK inhibitors. |
AID1822774 | Induction of apoptosis in human U-937 cells assessed as apoptosis rate at 5 uM measured after 48 hrs by AnnexinV-FITC staining based flow cytometry analysis relative to control (Rvb = 10.12 %) | | | |
AID1425002 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1772883 | Antiproliferative activity against human NCI-H322M cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors. |
AID1574160 | Cytotoxicity against human PBMC assessed as inhibition of cell proliferation at 30 uM after 72 hrs by CellTiter-Glo luminescent cell viability assay relative to control | 2019 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
| Synthesis and biological evaluation of novel 1-substituted 3-(3-phenoxyprop-1-yn-1-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amines as potent Bruton's tyrosine kinase (BTK) inhibitors. |
AID1772882 | Antiproliferative activity against human HL-60(TB) cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors. |
AID1822767 | Inhibition of BTK phosphorylation in human U-937 cells incubated for 4 hrs by Western blot assay | | | |
AID1418279 | Protein binding in rat plasma assessed as unbound fraction | 2018 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
| Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk. |
AID1623558 | Antiproliferative activity against human Raji cells at 5 uM up to 24 hrs by CCK8 assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ. |
AID1718985 | Inhibition of HCK (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 34 | Characterization of ibrutinib as a non-covalent inhibitor of SRC-family kinases. |
AID1615378 | Selectivity ratio of IC50 for HER2 (unknown origin) to IC50 for N-terminal His-tagged recombinant human BTK (393 to 659 residues) expressed in baculovirus infected Sf9 cells | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1587026 | Reversible inhibition of full-length human His-tagged BTK expressed in baculovirus expression system assessed as apparent dissociation half life by kinase tracer 236 based TR-FRET assay | 2019 | ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
| Aminopyrazole Carboxamide Bruton's Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning. |
AID1656331 | Inhibition of BTK in human whole blood cells after 120 mins by ELISA | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
| Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK). |
AID1424933 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1417603 | Clearance in mouse at 0.2 mg/kg, iv administered as single dose | 2018 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20
| Optimization of the efflux ratio and permeability of covalent irreversible BTK inhibitors. |
AID1870016 | Induction of apoptosis in human SU-DHL-6 cells assessed as late apoptotic cells at 1.5 uM incubated for 48 hrs by annexin V-FITC and PI staining based flow cytometry analysis (Rvb = 3.88 %) | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
| Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
AID629929 | Inhibition of ErbB1 relative to control | 2011 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
| Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis. |
AID1615370 | Inhibition of human HER4 using poly[Glu:Tyr] (4:1) as substrate preincubated for 60 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by filter binding method | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1560829 | Binding affinity to DNA-tagged recombinant JAK3 (unknown origin) measured after 1 hr by biotinylated-ligand affinity bead-based qPCR analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1424917 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424988 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1574154 | Antiproliferative activity against human Raji cells after 48 hrs by CCK8 assay | 2019 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
| Synthesis and biological evaluation of novel 1-substituted 3-(3-phenoxyprop-1-yn-1-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amines as potent Bruton's tyrosine kinase (BTK) inhibitors. |
AID1458988 | Efflux ratio of apparent permeability from basolateral side to apical side over apical side to basolateral side over in human Caco2 cells at 5 uM incubated for 2 hrs | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1673837 | Inhibition of full length human unphosphorylated BTK using FITC-Ahx-TSELKKVVALYDYMPMNAND-NH2 as substrate incubated for 60 mins in presence of ATP at Km concentration | 2019 | ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
| Design of Potent and Selective Covalent Inhibitors of Bruton's Tyrosine Kinase Targeting an Inactive Conformation. |
AID1424899 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1324664 | Cell cycle arrest in human Ramos cells assessed as accumulation at S phase at 10 uM by propidium iodide staining based flow cytometry (Rvb = 42.23%) | 2016 | ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
| Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing a |
AID1425123 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1499243 | Antiproliferative activity against human NCI-H1975 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1560823 | Binding affinity to DNA-tagged recombinant BMX (unknown origin) measured after 1 hr by biotinylated-ligand affinity bead-based qPCR analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1459011 | Kinetic solubility in Hepes buffer at 500 uM at pH 7.4 after 90 mins | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1725079 | Inhibition of human liver microsome CYP1A2 using phenacetin as substrate preincubated for 10 mins followed by substrate and NADPH addition and measured after 10 mins by LC-MS/MS analysis | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery and Evaluation of Pyrazolo[3,4- |
AID1656239 | Inhibition of BTK in human Ramos B cells assessed as reduction in BCR-stimulated calcium flux after 1 hr in dark condition measured for 180 sec | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
| Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK). |
AID1424909 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425154 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1714838 | Inhibition of recombinant human EGFR using Ulight-CAGAGAIETDKEYYTVKD as substrate incubate for 15 mins by LANCE assay | | | |
AID1424978 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1563040 | Induction of apoptosis in human Ramos cells assessed as necrotic cells at 5 uM measured after 15 mins by Annexin-V-APC staining-based flow cytometric analysis (Rvb = 1.50 %) | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines. |
AID1782001 | Selectivity index, ratio of IC50 for inhibition of ITK (unknown origin) to IC50 for inhibition of BTK (unknown origin) | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
| Discovery of 1-Amino-1 |
AID1591650 | Antiproliferative activity against human GRANTA-519 cells assessed as reduction in viability after 72 hrs by CellTiter-Glo luminescent assay | 2019 | Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
| Design, synthesis and biological evaluation of novel 2,3-indolinedione derivatives against mantle cell lymphoma. |
AID1417605 | Half life in mouse at 0.2 mg/kg, iv administered as single dose | 2018 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20
| Optimization of the efflux ratio and permeability of covalent irreversible BTK inhibitors. |
AID1738568 | Inhibition of EGFR (unknown origin) by ADP-Glo assay | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold. |
AID1538545 | Inhibition of MKK7 beta1 S273D/T275D double mutant (unknown origin) using JNK1 K55M mutant as substrate by ADP-Glo assay | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| Characterization of Covalent Pyrazolopyrimidine-MKK7 Complexes and a Report on a Unique DFG-in/Leu-in Conformation of Mitogen-Activated Protein Kinase Kinase 7 (MKK7). |
AID1334878 | Antiproliferative activity against human Ramos cells measured after 48 hrs by CCK-8 assay | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
| Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines. |
AID1469903 | Growth inhibition of human NB4 cells | | | |
AID1878122 | Binding affinity to TXK (unknown origin) assessed as dissociation constant by KINOMEscan analysis | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors. |
AID1878104 | Binding affinity to ERBB4 (unknown origin) assessed as dissociation constant by KINOMEscan analysis | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors. |
AID1738569 | Inhibition of ITK (unknown origin) by ADP-Glo assay | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold. |
AID1397239 | Induction of apoptosis in human NAMALWA cells assessed as morphological changes at 5 uM by acridine orange/ethidium bromide staining based phase contrast microscopic assay | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
| Novel amino acid-substituted diphenylpyrimidine derivatives as potent BTK inhibitors against B cell lymphoma cell lines. |
AID1469923 | Induction of apoptosis in human U2932 cells assessed as induction of PARP cleavage at 10 uM after 48 hrs by immunoblot | | | |
AID1425024 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424924 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1718984 | Inhibition of SRC (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 34 | Characterization of ibrutinib as a non-covalent inhibitor of SRC-family kinases. |
AID1458979 | Selectivity ratio of IC50 for wild type N-terminal GST-fused human EGFR cytoplasmic domain to IC50 for human recombinant GST-tagged EGFR L858R/T790M double mutant | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1425202 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1155522 | Cytotoxicity against human WSU-NHL cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity. |
AID719893 | Inhibition of recombinant Btk after 60 mins | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| Irreversible protein kinase inhibitors: balancing the benefits and risks. |
AID1615379 | Selectivity ratio of IC50 for human BLK to IC50 for N-terminal His-tagged recombinant human BTK (393 to 659 residues) expressed in baculovirus infected Sf9 cells | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1472055 | Toxicity in SCID CB.17 mouse xenografted with human OCI-LY10 cells assessed as change in body weight at 12 mg/kg, po qd after 34 days post inoculation measured on day 51 | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88 |
AID1418278 | Protein binding in mouse plasma assessed as unbound fraction | 2018 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
| Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk. |
AID1851530 | Antiproliferative activity against human MINO cells incubated for 72 hrs by CellTiter-Glo assay | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Design, synthesis, and biological evaluation of pyrrolopyrimidine derivatives as novel Bruton's tyrosine kinase (BTK) inhibitors. |
AID1425085 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1851523 | Selectivity ratio for inhibition of BTK (unknown origin) over EGFR (unknown origin) | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Design, synthesis, and biological evaluation of pyrrolopyrimidine derivatives as novel Bruton's tyrosine kinase (BTK) inhibitors. |
AID1524885 | Antiproliferative activity against human Maver1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell-titer-Glo luminescent cell viability assay | 2019 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
| Discovery of novel pyrazole derivatives as potential anticancer agents in MCL. |
AID1553437 | Inhibition of BTK in anti-IgM-stimulated human Ramos cells assessed as reduction in Akt phosphorylation at 10 uM incubated for 4 hrs followed by anti-IgM stimulation for 30 mins by Western blot analysis | 2019 | Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
| Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors. |
AID1870009 | Induction of cell cycle arrest in human DOHH-2 cells assessed as accumulation of cells at S phase at 1 uM incubated for 24 hrs by PI staining based flow cytometry analysis (Rvb = 55.11 %) | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
| Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
AID1397246 | Induction of apoptosis in human NAMALWA cells assessed as early apoptotic cells at 5 uM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0%) | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
| Novel amino acid-substituted diphenylpyrimidine derivatives as potent BTK inhibitors against B cell lymphoma cell lines. |
AID1469924 | Induction of apoptosis in human Pfeiffer cells assessed as induction of PARP cleavage at 10 uM after 48 hrs by immunoblot | | | |
AID1484561 | Induction of apoptosis in human Ramos cells assessed as early apoptotic cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric analysis relative to control | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design and synthesis of sulfonamide-substituted diphenylpyrimidines (SFA-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B-cell lymphoblastic leukemia. |
AID1425142 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1725083 | Half life in Sprague-Dawley rat at 2 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery and Evaluation of Pyrazolo[3,4- |
AID1725073 | AUC in BALB/c mouse 2 mg/kg, po measured upto 24 hrs by LC-MS/MS analysis | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery and Evaluation of Pyrazolo[3,4- |
AID1424904 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425040 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425147 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425082 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425129 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1549594 | Antiarthritic activity in DBA1/J mouse model of collagen-induced arthritis assessed as reduction in bone erosion at 12.5 mg/kg, po qd by H and E staining based assay | 2019 | European journal of medicinal chemistry, May-01, Volume: 169 | Design, synthesis and evaluation of novel 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as potent, selective and reversible Bruton's tyrosine kinase (BTK) inhibitors for the treatment of rheumatoid arthritis. |
AID1425021 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425036 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425188 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425203 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1560795 | Inhibition of full-length human recombinant BTK using FITC-Ahx-TSELKKVVALYDYMPMNAND-NH2 as substrate measured after 60 mins by caliper assay | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1615392 | Selectivity ratio of IC50 for TEC in HEK293 cells to IC50 for BTK in human Ramos cells | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1418291 | Oral bioavailability in mouse at 0.5 mg/kg | 2018 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
| Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk. |
AID1738554 | Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold. |
AID1638805 | Stability in mouse plasma assessed as compound remaining at 5 uM after 1 hr by LC/MS analysis | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors. |
AID1692287 | Inhibition of GP6 in human whole blood assessed as protein-mediated platelet aggregation preincubated for 15 mins followed by collagen stimulation and measured for 10 mins by multiple electrode aggregometry | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Progress toward a Glycoprotein VI Modulator for the Treatment of Thrombosis. |
AID1424595 | Inhibition of BTK (unknown origin) | 2017 | European journal of medicinal chemistry, Dec-15, Volume: 142 | Covalent binding design strategy: A prospective method for discovery of potent targeted anticancer agents. |
AID1424930 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425098 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1426145 | Induction of apoptosis in human Ramos cells assessed as early apoptotic cells at 10 uM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.7%) | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines. |
AID1425025 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1563023 | Antiproliferative activity against human Raji cells at 40 uM measured after 72 hrs by CCK-8 assay relative to control | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines. |
AID1869077 | Inhibition of BTK T474I mutant (unknown origin) expressed in baculovirus infected Trichoplusia ni pro cells incubated for 30 mins in presence of ATP by Microfluidic chip based mobility shift assay | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
| Medicinal Chemistry Strategies for the Development of Bruton's Tyrosine Kinase Inhibitors against Resistance. |
AID1425050 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1468848 | Inhibition of BTK (unknown origin) autophosphorylation at Y223 expressed in HEK293 cells at 1 uM by Western blot analysis | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
| Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development. |
AID1851556 | Toxicity in female CB-17 SCID nude mouse xenografted with human TMD8 cells assessed as effect on body weight at 25 mg/kg, po administered twice daily for 21 days | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Design, synthesis, and biological evaluation of pyrrolopyrimidine derivatives as novel Bruton's tyrosine kinase (BTK) inhibitors. |
AID1425197 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1304228 | Inhibition of BTK (unknown origin) assessed as reduction in phosphorylation of coumarin and fluorescein-labeled FRET peptide substrate incubated for 1 hr by Z-Lyte assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Structure-based discovery of novel 4,5,6-trisubstituted pyrimidines as potent covalent Bruton's tyrosine kinase inhibitors. |
AID1714866 | Inhibition of recombinant human FMS using Ulight-TK peptide as substrate incubate for 15 mins by LANCE assay | | | |
AID1615447 | Toxicity in NCG mouse xenografted with human OCI-LY10 cells assessed as effect on body weight at 2.5 to 7.5 mg/kg, po BID measured twice weekly | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1424974 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424911 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1399792 | Fraction unbound in rat plasma | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
| Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit. |
AID1465443 | Selectivity ratio of IC50 for TEC (unknown origin) to IC50 for BTK (unknown origin) | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| In Silico Identification of a Novel Hinge-Binding Scaffold for Kinase Inhibitor Discovery. |
AID1425014 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1725088 | AUC (0 to last) in Sprague-Dawley rat at 10 mg/kg, po measured upto 24 hrs by LC-MS/MS analysis | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery and Evaluation of Pyrazolo[3,4- |
AID1469896 | Growth inhibition of human SU-DHL-2 cells | | | |
AID1822784 | Antitumor activity against human U-937 cells xenografted in Balb/c nude mouse assessed as tumor growth inhibition at 25 mg/kg, po administered once daily for 14 days | | | |
AID1563079 | Inhibition of BTK in anti-IgM-stimulated human Ramos cells assessed as decrease in auto-phosphorylation at Y223 residue at 0.1 to 5 uM after 48 hrs by Western blot analysis | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines. |
AID1650549 | Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | 2020 | Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
| Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors. |
AID1424963 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1324656 | Inhibition of recombinant human N-terminal His-tagged BTK expressed in baculovirus infected sf9 cells using poly(4:1 Glu,Tyr) as substrate by ADP-Glo kinase assay | 2016 | ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
| Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing a |
AID1623564 | Induction of apoptosis in human Ramos cells assessed as necrotic cells at 5 uM after 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometric analysis (Rvb = 1.11%) | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ. |
AID1851554 | Antitumor activity against human TMD8 cells xenografted in female CB-17 SCID nude mouse assessed as tumor growth inhibition at 25 mg/kg, po administered twice daily for 21 days | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Design, synthesis, and biological evaluation of pyrrolopyrimidine derivatives as novel Bruton's tyrosine kinase (BTK) inhibitors. |
AID1878120 | Binding affinity to JAK3 (unknown origin) assessed as dissociation constant by KINOMEscan analysis | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors. |
AID1560832 | Selectivity ratio of Kd for DNA-tagged recombinant ITK (unknown origin) to Kd for DNA-tagged recombinant BTK (unknown origin) | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1425148 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1692289 | Inhibition of human platelet lamellipodia formation on CRP-XL 1 umol/L preincubated for 4 mins followed by CRP-XL addition and measured after 45 mins (Rvb = 69%) | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Progress toward a Glycoprotein VI Modulator for the Treatment of Thrombosis. |
AID1418294 | Intrinsic clearance in human microsomes | 2018 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
| Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk. |
AID1499254 | Antiproliferative activity against human U937 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1425001 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425169 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424892 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1615388 | Inhibition of ITK in human Jurkat cells assessed as reduction in PLCgamma1 phosphorylation at Y783 residues preincubated for 2 hrs followed by H2O2 addition and measured after 10 mins by Western blot analysis | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1424997 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1499230 | Inhibition of TEL-fused EGFR (unknown origin) expressed in mouse BA/F3 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1714842 | Inhibition of recombinant human JAK3 using Ulight-CAGAGAIETDKEYYTVKD as substrate incubate for 60 mins by LANCE assay | | | |
AID1822768 | Inhibition of ITK phosphorylation in human Jurkat cells incubated for 4 hrs by Western blot assay | | | |
AID1587024 | Reversible inhibition of full-length human His-tagged BTK expressed in baculovirus expression system assessed as ratio of Kinact to Ki by kinase tracer 236 based TR-FRET assay | 2019 | ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
| Aminopyrazole Carboxamide Bruton's Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning. |
AID1563054 | Induction of apoptosis in human Raji cells assessed as early apoptotic cells at 5 uM measured after 15 mins by Annexin-V-APC staining-based flow cytometric analysis (Rvb = 0.021 %) | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines. |
AID1851532 | Antiproliferative activity against human Ramos cells incubated for 72 hrs by CellTiter-Glo assay | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Design, synthesis, and biological evaluation of pyrrolopyrimidine derivatives as novel Bruton's tyrosine kinase (BTK) inhibitors. |
AID1656240 | Half life in human liver microsomes in presence of NAPDH | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
| Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK). |
AID1424935 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1375528 | Inhibition of recombinant human ITK using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
AID1425199 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1324659 | Induction of apoptosis in human Ramos cells assessed as viable cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry relative to control | 2016 | ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
| Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing a |
AID1591627 | Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | 2019 | Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
| Discovery and Biological evaluation of pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione derivatives as potent Bruton's tyrosine kinase inhibitors. |
AID1458992 | Intrinsic clearance in mouse liver microsomes at 3 uM after 50 mins by LC-MS method | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1424891 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1468805 | Inhibition of recombinant human full length His-tagged BLK expressed in baculovirus at 1 uM by Z'-LYTE assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
| Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development. |
AID1718990 | Inhibition of BTK (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 34 | Characterization of ibrutinib as a non-covalent inhibitor of SRC-family kinases. |
AID1889499 | Inhibition of EGFR (unknown origin) by lanthascreen Tb kinase activity assay | 2022 | Journal of natural products, 02-25, Volume: 85, Issue:2
| Ophiorrhines F and G, Key Biogenetic Intermediates of Ophiorrhine Alkaloids from |
AID1527035 | Antitumor activity against human OCI-LY10 cells xenografted in CB.17 SCID mouse assessed as induction of tumor stasis at 12 mg/kg, po QD dosed 34 days after tumor cell inoculation | | | |
AID1418272 | Inhibition of recombinant human full length N-terminal GST-tagged BTK (2 to 659 residues) expressed in baculovirus expression system using FITC-AHA-EEPLYWSFPAKKK-NH2 substrate measured after 90 mins by off-chip mobility shift assay | 2018 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
| Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk. |
AID1426141 | Antiproliferative activity against human Ramos cells after 48 hrs by CCK-8 assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines. |
AID1468803 | Inhibition of cytoplasmic recombinant human full length His-tagged BMX expressed in baculovirus at 1 uM by Z'-LYTE assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
| Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development. |
AID1563080 | Inhibition of BTK in anti-IgM-stimulated human Raji cells assessed as decrease in auto-phosphorylation at Y223 residue at 0.1 to 5 uM after 48 hrs by Western blot analysis | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines. |
AID1425176 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1417606 | Oral bioavailability in mouse at 0.5 mg/kg administered as cassette dosing | 2018 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20
| Optimization of the efflux ratio and permeability of covalent irreversible BTK inhibitors. |
AID1425149 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425201 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1563069 | Cell cycle arrest in human Raji cells assessed as accumulation at G0/G1 phase at 1 uM measured after 48 hrs by propidium iodide/RNase staining based flow cytometric analysis (Rvb = 48.68 %) | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines. |
AID1469898 | Growth inhibition of human U2932 cells | | | |
AID1425212 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1468804 | Inhibition of human full length GST-tagged TXK expressed in baculovirus at 1 uM by Z'-LYTE assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
| Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development. |
AID1239424 | Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by cell titer glo assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Development of Selective Covalent Janus Kinase 3 Inhibitors. |
AID1527028 | Growth inhibition of human OCI-LY19 cells at 0.3 nM incubated for 3 days by Alamar blue dye based fluorescence assay (Rvb = 3%) | | | |
AID1375529 | Inhibition of recombinant human RET using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
AID1425013 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424942 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1458980 | Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1623568 | Cell cycle arrest in human Ramos cells assessed as accumulation at G2/M phase at 5 uM after 48 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 4.26%) | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ. |
AID1469894 | Reversible inhibition of full length recombinant human N-terminal His tagged BKT expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 2 to 60 mins followed by substrate addition after 1 hr by ADP-Glo lumin | | | |
AID1725087 | AUC (0 to last) in Sprague-Dawley rat at 2 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery and Evaluation of Pyrazolo[3,4- |
AID1772876 | Antiproliferative activity against human SK-MEL-5 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors. |
AID1553408 | Antiproliferative activity against human Raji cells assessed as reduction in cell growth incubated for 48 hrs by MTS assay | 2019 | Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
| Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors. |
AID1424922 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1391148 | Inhibition of full length human N-terminal GST-tagged BTK (2 to 659 residues) expressed in baculovirus expression system using biotinylated substrate after 50 mins by HTRF assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Design, synthesis and biological evaluation of novel 3-substituted pyrazolopyrimidine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors. |
AID1718988 | Inhibition of SRC T338M mutant (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 34 | Characterization of ibrutinib as a non-covalent inhibitor of SRC-family kinases. |
AID1425187 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1638811 | Efflux ratio of apparent permeability in human Caco2 cells at 5 uM after 2 hrs by transwell membrane based assay | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors. |
AID671743 | Inhibition of BMX | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies. |
AID1714837 | Inhibition of BLK (unknown origin) | | | |
AID1468802 | Inhibition of recombinant human full length His-tagged BTK expressed in baculovirus at 1 uM by Z'-LYTE assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
| Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development. |
AID1397235 | Antiproliferative activity against human Ramos cells after 72 hrs by CCK8 assay | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
| Novel amino acid-substituted diphenylpyrimidine derivatives as potent BTK inhibitors against B cell lymphoma cell lines. |
AID1574153 | Antiproliferative activity against human Ramos cells after 48 hrs by CCK8 assay | 2019 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
| Synthesis and biological evaluation of novel 1-substituted 3-(3-phenoxyprop-1-yn-1-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amines as potent Bruton's tyrosine kinase (BTK) inhibitors. |
AID1878127 | Selectivity index, ratio of Kd for ITK (unknown origin) to Kd for BTK (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors. |
AID1872692 | Antitumor activity against human DOHH-2 cells xenografted in CB17/SCID mouse assessed as reduction in tumor growth at 15 mg/kg, po administered once daily in combination with idelalisib at 25 mg/kg for 30 days and measured twice a week relative to control | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Recent development of BTK-based dual inhibitors in the treatment of cancers. |
AID1725094 | Oral bioavailability in BALB/c mouse at 2 mg/kg measured upto 24 hrs by LC-MS/MS analysis | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery and Evaluation of Pyrazolo[3,4- |
AID1425018 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1469909 | Effect on BTK transphosphorylation at PLCgamma1 Y783 in human U2932 cells up to 1 uM measured after 4 hrs by chemiluminescent assay | | | |
AID1571253 | Induction of apoptosis in human Ramos cells assessed as early apoptotic cells at 5 uM after 48 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 1.08%) | | | |
AID1155520 | Cytotoxicity against human Pfeiffer cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity. |
AID1615437 | Antitumor activity against human OCI-LY10 cells xenografted in NCG mouse assessed as tumor growth inhibition at 7.5 mg/kg, po BID measured on day 28 by caliper method relative to control | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1673832 | Inhibition of ERBB4 (unknown origin) | 2019 | ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
| Design of Potent and Selective Covalent Inhibitors of Bruton's Tyrosine Kinase Targeting an Inactive Conformation. |
AID1499251 | Antiproliferative activity against human Ramos cells after 72 hrs by CellTiter-Glo assay | | | |
AID1615436 | Antitumor activity against human OCI-LY10 cells xenografted in NCG mouse assessed as tumor growth inhibition at 2.5 mg/kg, po BID measured on day 28 by caliper method relative to control | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1526952 | Inhibition of IRAK4 in human OCI-LY10 cells assessed as decrease in pIKBalpha levels incubated for 14 hrs by Western blotting analysis | | | |
AID1425039 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1822763 | Inhibition of human ITK using poly-Glu-Tyr (4:1) as substrate incubated for 1 hr by ELISA | | | |
AID1425009 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1656256 | Inhibition of HER1 (unknown origin) | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
| Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK). |
AID1871764 | Inhibition of BMX (unknown origin) | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Review of the development of BTK inhibitors in overcoming the clinical limitations of ibrutinib. |
AID1425130 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1615382 | Selectivity ratio of IC50 for human HER4 to IC50 for N-terminal His-tagged recombinant human BTK (393 to 659 residues) expressed in baculovirus infected Sf9 cells | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1399784 | Efflux ratio of permeability in human Caco2 cells | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
| Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit. |
AID1424998 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1889497 | Inhibition of ITK (unknown origin) by lanthascreen Tb kinase activity assay | 2022 | Journal of natural products, 02-25, Volume: 85, Issue:2
| Ophiorrhines F and G, Key Biogenetic Intermediates of Ophiorrhine Alkaloids from |
AID1324660 | Induction of apoptosis in human Ramos cells assessed as early apoptotic cells at 10 uM after 48 hrs by annexin V/FITC propidium iodide staining based flow cytometry relative to control | 2016 | ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
| Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing a |
AID1878119 | Binding affinity to ITK (unknown origin) assessed as dissociation constant by KINOMEscan analysis | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors. |
AID1425083 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1475900 | Cytotoxicity against human Mino cells assessed as reduction in cell survival at 25 uM after 48 hrs by Annexin V/propidium iodide based flow cytometric analysis | 2017 | Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
| Anchimerically Activated ProTides as Inhibitors of Cap-Dependent Translation and Inducers of Chemosensitization in Mantle Cell Lymphoma. |
AID1334888 | Cell cycle arrest in human Ramos cells assessed as accumulation at S phase at 10 uM measured after 48 hrs by propidium iodide based flow cytometry (Rvb = 55.07 %) | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
| Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines. |
AID1425175 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1673826 | Inhibition of BTK in human whole blood assessed as reduction in polyclonal anti-IgM antibody/human IL4-stimulated CD69 cell surface expression on B cells incubated for 16 hrs by FACS analysis | 2019 | ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
| Design of Potent and Selective Covalent Inhibitors of Bruton's Tyrosine Kinase Targeting an Inactive Conformation. |
AID1587022 | Inhibition of full-length human His-tagged BTK expressed in baculovirus expression system using FAM-Srctide peptide as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr by TR-FRET Lanthascreen assay | 2019 | ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
| Aminopyrazole Carboxamide Bruton's Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning. |
AID1714833 | Inhibition of BMX (unknown origin) | | | |
AID1425180 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1718993 | Inhibition of EGFR T790M mutant (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 34 | Characterization of ibrutinib as a non-covalent inhibitor of SRC-family kinases. |
AID1417599 | Inhibition of human ERG | 2018 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20
| Optimization of the efflux ratio and permeability of covalent irreversible BTK inhibitors. |
AID1425022 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1560797 | Inhibition of BTK in human B cells assessed as reduction in anti-IgM/IL4-stimulated CD69 expression on B cells preincubated for 60 mins followed by anti-IgM antibody/IL4 stimulation and measured after 16 hrs by flow cytometry | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1830232 | Inhibition of BTK in human Ramos cells assessed as reduction of IgM stimulated PLCgamma2 (Y1217) phosphorylation after 24 hrs by western blot assay | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
| Discovery of AS-1763: A Potent, Selective, Noncovalent, and Orally Available Inhibitor of Bruton's Tyrosine Kinase. |
AID1499262 | Antiproliferative activity against human HL60 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1871765 | Inhibition of EGFR (unknown origin) | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Review of the development of BTK inhibitors in overcoming the clinical limitations of ibrutinib. |
AID1638804 | Stability in human plasma assessed as compound remaining at 5 uM after 1 hr by LC/MS analysis | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors. |
AID1560824 | Binding affinity to DNA-tagged recombinant TEC (unknown origin) measured after 1 hr by biotinylated-ligand affinity bead-based qPCR analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1650553 | Antiproliferative activity against human OCI-LY10 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | 2020 | Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
| Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors. |
AID1725076 | Protein binding in mouse plasma at 2 uM incubated for 4 hrs by LC-MS/MS analysis | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery and Evaluation of Pyrazolo[3,4- |
AID1714843 | Inhibition of JAK1 (unknown origin) | | | |
AID1324658 | Antiproliferative activity against human Raji cells after 48 hrs by CCK-8 assay | 2016 | ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
| Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing a |
AID1418276 | Inhibition of BTK in human whole blood | 2018 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
| Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk. |
AID1880138 | Inhibition of EGFR (unknown origin) | 2022 | Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8
| The Ascension of Targeted Covalent Inhibitors. |
AID1425023 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1401316 | Cytotoxicity against human PBMCs assessed as induction of morphological changes at <10 uM after 24 hrs by AO/PI staining-based phase contrast microscopy | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma. |
AID1425200 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1401318 | Induction of apoptosis in human Ramos cells assessed as late apoptotic cells at 10 uM after 72 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.5%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma. |
AID1472048 | Growth inhibition of human SUDHL2 cells at 0.0003 uM after 3 days by AlamarBlue assay (Rvb = - 1 %) | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88 |
AID1738552 | Inhibition of BTK (unknown origin) at 100 nM by ADP-Glo assay relative to control | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold. |
AID1870014 | Induction of apoptosis in human SU-DHL-6 cells assessed as viable cells at 1.5 uM incubated for 48 hrs by annexin V-FITC and PI staining based flow cytometry analysis (Rvb = 87.0 %) | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
| Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
AID1419872 | Toxicity in SCID CB.17 mouse xenografted with human OCI-LY10 cells harboring MyD88 L256P/CD79MUT double mutant assessed as body weight loss at 12 mg/kg, po qd after 43 days (Rvb = 2%) | 2018 | Bioorganic & medicinal chemistry, 02-15, Volume: 26, Issue:4
| Optimization of permeability in a series of pyrrolotriazine inhibitors of IRAK4. |
AID1401307 | Inhibition of recombinant full-length N-terminal His-tagged human BTK expressed in baculovirus infected Sf9 insect cells using Poly(4:1 Glu,Tyr) peptide substrate incubated for 60 mins by ADP-Glo luminescence assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma. |
AID1725091 | Clearance in BALB/c mouse at 1 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery and Evaluation of Pyrazolo[3,4- |
AID1524887 | Antiproliferative activity against human Mino cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell-titer-Glo luminescent cell viability assay | 2019 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
| Discovery of novel pyrazole derivatives as potential anticancer agents in MCL. |
AID1425179 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1418293 | Induction of CYP3A4 mRNA expression in hepatocytes (unknown origin) | 2018 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
| Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk. |
AID1425084 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1324662 | Induction of apoptosis in human Ramos cells assessed as necrotic cells at 10 uM after 48 hrs by annexin V/FITC propidium iodide staining based flow cytometry relative to control | 2016 | ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
| Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing a |
AID1478518 | Cytotoxicity against human NCI-H1975 cells assessed as decrease in cell viability after 72 hrs by CellTiter-Glo assay | 2017 | Bioorganic & medicinal chemistry, 06-01, Volume: 25, Issue:11
| Identification of spirobisnaphthalene derivatives with anti-tumor activities from the endophytic fungus Rhytidhysteron rufulum AS21B. |
AID1638802 | Apparent permeability across apical to basolateral side in MDCK2-MDR1 cells at 10 uM after 2 hrs by transwell membrane based assay | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors. |
AID1871763 | Inhibition of TXK (unknown origin) | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Review of the development of BTK inhibitors in overcoming the clinical limitations of ibrutinib. |
AID1425165 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1591653 | Antiproliferative activity against human Maver1 cells assessed as reduction in viability after 72 hrs by CellTiter-Glo luminescent assay | 2019 | Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
| Design, synthesis and biological evaluation of novel 2,3-indolinedione derivatives against mantle cell lymphoma. |
AID1425124 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425144 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1155533 | Plasma concentration in CB17 SCID mouse xenografted with human DOHH2 cells at 10 mg/kg, iv qd administered for 14 days measured at 2 hrs post last dose | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity. |
AID1418290 | Inhibition of CYP3A4 (unknown origin) | 2018 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
| Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk. |
AID1470409 | Induction of apoptosis in human Pfeiffer cells assessed as induction of caspase-3 cleavage at 10 uM after 48 hrs by immunoblot | | | |
AID1499274 | Antiproliferative activity against primary CLL cells derived from p15 patient after 72 hrs by CellTiter-Glo assay | | | |
AID1714877 | Inhibition of SYK (unknown origin) | | | |
AID1425177 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1458976 | Inhibition of wild type N-terminal GST-fused human EGFR cytoplasmic domain expressed in baculovirus expression system preincubated for 30 mins followed by ATP and TK-substrate addition measured after 25 mins by HTRF assay | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1417607 | Inhibition of BTK in human PBMC | 2018 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20
| Optimization of the efflux ratio and permeability of covalent irreversible BTK inhibitors. |
AID1870001 | Induction of cell cycle arrest in human SU-DHL-6 cells assessed as accumulation of cells at S phase at 0.5 uM incubated for 24 hrs by PI staining based FACScan flow cytometry analysis (Rvb = 24.18 %) | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
| Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
AID1656257 | Inhibition of HER4 (unknown origin) | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
| Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK). |
AID1772878 | Antiproliferative activity against human UO-31 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors. |
AID1375518 | Antiproliferative activity against human TMD8 cells after 72 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
AID1871761 | Inhibition of TEC (unknown origin) | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Review of the development of BTK inhibitors in overcoming the clinical limitations of ibrutinib. |
AID1155511 | Inhibition of Btk phosphorylation at Tyr551 in human Ramos cells after 1 hr by Western blot analysis | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity. |
AID1425208 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425073 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1475908 | Inhibition of 4EBP1 phosphorylation at Thr 37/46 residues in human Mino cells at 10 to 25 uM after 48 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
| Anchimerically Activated ProTides as Inhibitors of Cap-Dependent Translation and Inducers of Chemosensitization in Mantle Cell Lymphoma. |
AID1524886 | Antiproliferative activity against human Z138 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell-titer-Glo luminescent cell viability assay | 2019 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
| Discovery of novel pyrazole derivatives as potential anticancer agents in MCL. |
AID1425143 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1650554 | Metabolic stability in human liver microsomes assessed as half life at 0.2 uM incubated for 60 mins by UPLC-MS/MS analysis | 2020 | Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
| Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors. |
AID1375524 | Inhibition of recombinant human ErbB4 using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
AID1425164 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1499267 | Antiproliferative activity against human K562 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1425133 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1401320 | Induction of apoptosis in human Ramos cells assessed as viable cells at 10 uM after 72 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 98.7%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma. |
AID1549551 | Antiproliferative activity against human JeKo1 cells | 2019 | European journal of medicinal chemistry, May-01, Volume: 169 | Design, synthesis and evaluation of novel 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as potent, selective and reversible Bruton's tyrosine kinase (BTK) inhibitors for the treatment of rheumatoid arthritis. |
AID1530075 | Inhibition of BTK (unknown origin) | 2018 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
| Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy. |
AID1878123 | Selectivity index, ratio of Kd for BMX (unknown origin) to Kd for BTK (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors. |
AID1527032 | Growth inhibition of human OCI-LY19 cells at 42 nM incubated for 3 days by Alamar blue dye based fluorescence assay (Rvb = 3%) | | | |
AID1324663 | Cell cycle arrest in human Ramos cells assessed as accumulation at G0/G1 phase at 10 uM by propidium iodide staining based flow cytometry (Rvb = 56.19%) | 2016 | ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
| Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing a |
AID1638800 | Apparent permeability across apical to basolateral side in human Caco2 cells at 5 uM after 2 hrs by transwell membrane based assay | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors. |
AID1738573 | Inhibition of BTK in human TMD8 cells assessed as reduction in cell proliferation at 10 uM measured upto 60 hrs by CCK-8 assay | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold. |
AID1499258 | Antiproliferative activity against human MOLM16 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1673812 | In vivo protein occupancy at BTK in Wistar Han rat spleen assessed as BTK level in plasma at 10 mg/kg, po measured after 2 hrs | 2019 | ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
| Design of Potent and Selective Covalent Inhibitors of Bruton's Tyrosine Kinase Targeting an Inactive Conformation. |
AID1425053 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1615345 | Inhibition of EGFR (unknown origin) preincubated for 1 hr followed by Biotin-AVLESEEELYSSARQ-NH2 substrate addition in presence of ATP and measured after 1 hr by TR-FRET assay | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1615363 | Inhibition of human BTK using poly[Glu:Tyr] (4:1) as substrate preincubated for 60 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by filter binding method | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1499263 | Antiproliferative activity against human CMK cells after 72 hrs by CellTiter-Glo assay | | | |
AID1720524 | Inhibition of recombinant full length human GST-tagged ITK expressed in baculovirus expression system using tyrosine-1 peptide as substrate preincubated for 1 hr in presence of ATP by Z'-LYTE assay | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
| Discovery of quinoline-based irreversible BTK inhibitors. |
AID1472049 | Growth inhibition of human SUDHL2 cells at 0.001 uM after 3 days by AlamarBlue assay (Rvb = - 1 %) | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88 |
AID1638798 | Kinetic solubility of the compound in Hepes buffer at pH 7.4 after 90 mins | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors. |
AID1425028 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1571246 | Antiproliferative activity against human Raji cells after 48 hrs by MTT assay | | | |
AID1488737 | Inhibition of EGFR (unknown origin) | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
| Discovery of (R)-5-(benzo[d][1,3]dioxol-5-yl)-7-((1-(vinylsulfonyl)pyrrolidin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (B6) as a potent Bmx inhibitor for the treatment of NSCLC. |
AID1425030 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425095 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1397236 | Antiproliferative activity against human Raji cells after 72 hrs by CCK8 assay | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
| Novel amino acid-substituted diphenylpyrimidine derivatives as potent BTK inhibitors against B cell lymphoma cell lines. |
AID1425051 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1560833 | Selectivity ratio of Kd for DNA-tagged recombinant EGFR (unknown origin) to Kd for DNA-tagged recombinant BTK (unknown origin) | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1869075 | Inhibition of BTK C481S mutant (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 30 mins in presence of ATP by Microfluidic chip based mobility shift assay | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
| Medicinal Chemistry Strategies for the Development of Bruton's Tyrosine Kinase Inhibitors against Resistance. |
AID1499246 | Antiproliferative activity against human RV1 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1418296 | Intrinsic clearance in rat microsomes | 2018 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
| Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk. |
AID1615369 | Inhibition of human BRK using poly[Glu:Tyr] (4:1) as substrate preincubated for 60 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by filter binding method | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1615362 | Antiproliferative activity against human OCI-LY10 cells after 6 days by Celltiter-glo luminescent cell viability assay | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1880539 | Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay | 2022 | Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
| Structural Feature Analyzation Strategies toward Discovery of Orally Bioavailable PROTACs of Bruton's Tyrosine Kinase for the Treatment of Lymphoma. |
AID1425087 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424919 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425045 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424980 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425100 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425204 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425103 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1574155 | Antiproliferative activity against human DOHH2 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
| Synthesis and biological evaluation of novel 1-substituted 3-(3-phenoxyprop-1-yn-1-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amines as potent Bruton's tyrosine kinase (BTK) inhibitors. |
AID1875918 | Inhibition of BTK (unknown origin) | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
AID1499236 | Inhibition of TEL-fused JAK2 (unknown origin) expressed in mouse BA/F3 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1425150 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1563056 | Induction of apoptosis in human Raji cells assessed as necrotic cells at 5 uM measured after 15 mins by Annexin-V-APC staining-based flow cytometric analysis (Rvb = 1.87 %) | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines. |
AID1725071 | Inhibition of recombinant human His-tagged full length BTK expressed in baculovirus expression system using TK1 as substrate incubated for 60 mins by HTRF assay | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery and Evaluation of Pyrazolo[3,4- |
AID1870006 | Induction of cell cycle arrest in human DOHH-2 cells assessed as accumulation of cells at G0/G1 phase at 1 uM incubated for 24 hrs by PI staining based flow cytometry analysis (Rvb = 23.47 %) | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
| Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
AID1469914 | Effect on BTK transphosphorylation at PLCgamma1 Y783 in human Pfeiffer cells up to 1 uM measured after 4 hrs by chemiluminescent assay | | | |
AID1469905 | Growth inhibition of human M07e cells | | | |
AID1469893 | Reversible inhibition of full length recombinant human N-terminal His tagged BKT expressed in baculovirus infected Sf9 insect cells assessed as inactivation rate using poly (Glu,Tyr)4:1 as substrate pretreated for 2 to 60 mins followed by substrate additi | | | |
AID1425125 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425205 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1894186 | Antiproliferative activity against anti-IgM-stimulated human KB cells assessed as cell growth inhibition pretreated for 30 mins followed by anti-IgM stimulation for 72 hrs by celltiter-glo reagent based assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application. |
AID1419869 | Antitumor activity against human OCI-LY10 cells harboring MyD88 L256P/CD79MUT double mutant xenografted in SCID CB.17 mouse assessed as tumor growth inhibition at 12 mg/kg, po qd after 43 days relative to control | 2018 | Bioorganic & medicinal chemistry, 02-15, Volume: 26, Issue:4
| Optimization of permeability in a series of pyrrolotriazine inhibitors of IRAK4. |
AID1880140 | Inhibition of EGFR phosphorylation in human A-431 cells | 2022 | Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8
| The Ascension of Targeted Covalent Inhibitors. |
AID1155508 | Inhibition of EGFR (unknown origin) at 5 nM after 1 hr by HTRF assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity. |
AID1889498 | Inhibition of TEC (unknown origin) by lanthascreen Tb kinase activity assay | 2022 | Journal of natural products, 02-25, Volume: 85, Issue:2
| Ophiorrhines F and G, Key Biogenetic Intermediates of Ophiorrhine Alkaloids from |
AID1399801 | Half life in rat at 0.5 mg/kg, po | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
| Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit. |
AID1880139 | Inhibition of BTK in human whole blood | 2022 | Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8
| The Ascension of Targeted Covalent Inhibitors. |
AID1587027 | Cytotoxicity against human THLE cells | 2019 | ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
| Aminopyrazole Carboxamide Bruton's Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning. |
AID1425122 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1623552 | Antiproliferative activity against human Raji cells after 48 hrs by CCK8 assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ. |
AID1155535 | Antitumor activity against human DOHH2 cells xenografted in CB17 SCID mouse assessed as tumor growth inhibition at 10 mg/kg, iv qd administered for 14 days measured over 14 days of compound treatment relative to vehicle-treated control | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity. |
AID1615383 | Selectivity ratio of IC50 for human FGR to IC50 for N-terminal His-tagged recombinant human BTK (393 to 659 residues) expressed in baculovirus infected Sf9 cells | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1426156 | Cell cycle arrest in human Ramos cells assessed as accumulation at G0/G1 phase at 10 uM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 56.19%) | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines. |
AID1591649 | Antiproliferative activity against human Mino cells assessed as reduction in viability after 72 hrs by CellTiter-Glo luminescent assay | 2019 | Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
| Design, synthesis and biological evaluation of novel 2,3-indolinedione derivatives against mantle cell lymphoma. |
AID1425003 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1560830 | Selectivity ratio of Kd for DNA-tagged recombinant BMX (unknown origin) to Kd for DNA-tagged recombinant BTK (unknown origin) | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1880135 | Inhibition of BTK (unknown origin) | 2022 | Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8
| The Ascension of Targeted Covalent Inhibitors. |
AID1425006 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1499256 | Antiproliferative activity against human MOLM13 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1878102 | Binding affinity to ERBB2 (unknown origin) assessed as dissociation constant by KINOMEscan analysis | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors. |
AID1782002 | Selectivity index, ratio of IC50 for inhibition of EGFR (unknown origin) to IC50 for inhibition of BTK (unknown origin) | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
| Discovery of 1-Amino-1 |
AID1587023 | Inhibition of human EGFR cytoplasmic domain expressed in baculovirus expression system using FITC-C6-KKAEEEEYFELVAKK-NH2 as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr by TR-FRET Lanthascreen assay | 2019 | ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
| Aminopyrazole Carboxamide Bruton's Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning. |
AID1424940 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1334900 | Induction of apoptosis in human Ramos cells assessed as necrotic cells at 10 uM measured after 48 hrs by Annexin V-FITC/propidium iodide based flow cytometry (Rvb = 0.2 %) | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
| Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines. |
AID1418285 | Inhibition of CYP2C9 (unknown origin) | 2018 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
| Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk. |
AID1673923 | Inhibition of BTK C481S (unknown origin) | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19
| Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations. |
AID1499261 | Antiproliferative activity against human NB4 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1424956 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425161 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1880136 | Inhibition of TEC (unknown origin) | 2022 | Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8
| The Ascension of Targeted Covalent Inhibitors. |
AID1425155 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1656330 | Inhibition of BTK in human whole blood cells after 30 mins by ELISA | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
| Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK). |
AID1772873 | Antiproliferative activity against human MOLT-4 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors. |
AID1425117 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425097 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425174 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1469916 | Inhibition of BTK transphosphorylation at PLCgamma2 Y1217 in human Pfeiffer cells up to 1 uM measured after 4 hrs by chemiluminescent assay | | | |
AID1469887 | Inhibition of full length recombinant human N-terminal His tagged BKT expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 60 mins followed by substrate addition after 1 hr by ADP-Glo luminescence assay | | | |
AID1425075 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1472007 | Inhibition of IRAK4 in human OCI-LY10 cells harboring MYD88 mutation assessed as reduction in IKBalpha phosphorylation at 3 nM after 14 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88 |
AID1155512 | Inhibition of Btk in human Ramos cells assessed as inhibition of PLC-gamma2 phosphorylation at Tyr1217 after 1 hr by Western blot analysis | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity. |
AID1424939 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1738572 | Inhibition of BTK in human TMD8 cells assessed as reduction in cell proliferation incubated for 24 hrs by CCK-8 assay | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold. |
AID1571248 | Inhibition of human recombinant full-length BTK at 100 nM using poly (4:1 Glu, Tyr) peptide substrate after 60 mins by ADP-Glo assay relative to control | | | |
AID1822771 | Selectivity ratio of IC50 for inhibition of EGFR phosphorylation in human A549 cells to IC50 for inhibition of BTK phosphorylation in human U-937 cells | | | |
AID1563037 | Induction of apoptosis in human Ramos cells assessed as viable cells at 5 uM measured after 15 mins by Annexin-V-APC staining-based flow cytometric analysis (Rvb = 96.5 %) | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines. |
AID671741 | Inhibition of human BTK by enzymatic assay | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies. |
AID1425102 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425158 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1426157 | Cell cycle arrest in human Ramos cells assessed as accumulation at S phase at 10 uM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 42.23%) | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines. |
AID1782037 | Antitumor activity against human TMD8 cells xenografted in CB-17 SCID nude mouse assessed as tumor growth inhibition at 7.5 mg/kg, po bid administered for 21 days | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
| Discovery of 1-Amino-1 |
AID1424971 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425209 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1375537 | Inhibition of BTK in human TMD8 cells assessed as decrease in PLCgamma2 phosphorylation at Y759 at 1 uM after 4 hrs by Western blot method | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
AID1499259 | Antiproliferative activity against human HEL cells after 72 hrs by CellTiter-Glo assay | | | |
AID1465442 | Inhibition of TEC (unknown origin) after 2 hrs by LanthaScreen assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| In Silico Identification of a Novel Hinge-Binding Scaffold for Kinase Inhibitor Discovery. |
AID1425049 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424964 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424908 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1476269 | Antiproliferative activity against mouse BAF3 cells harboring FLT3-ITD mutation after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
AID1571245 | Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay | | | |
AID1499245 | Antiproliferative activity against human DU145 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1591630 | Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | 2019 | Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
| Discovery and Biological evaluation of pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione derivatives as potent Bruton's tyrosine kinase inhibitors. |
AID1553436 | Inhibition of BTK in anti-IgM-stimulated human Ramos cells assessed as reduction in Erk phosphorylation at 10 uM incubated for 4 hrs followed by anti-IgM stimulation for 30 mins by Western blot analysis | 2019 | Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
| Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors. |
AID1424900 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1401311 | Antiproliferative activity against human NAMALWA cells after 72 hrs by CCK-8 assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma. |
AID1424947 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1481309 | Inhibition of EGFR exon 19 deletion mutant in human PC9 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1399802 | Oral bioavailability in rat at 0.5 mg/kg | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
| Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit. |
AID1781999 | Inhibition of N-terminal DYKDDDD-tagged EGFR (669 to 1210 residues) (unknown origin) expressed in Sf21 insect cells using NH2-ETVYSEVRK-biotin as substrate preincubated for 1 hr followed by ATP addition and measured after 2 hrs by ELISA | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
| Discovery of 1-Amino-1 |
AID1656244 | Inhibition of His-tagged BTK (unknown origin) after 1.5 hrs by HTRF analysis | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
| Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK). |
AID1460483 | Antiviral activity against Dengue virus serotype 2 strain New Guinea C infected in HuH7 cells at 2.5 to 10 uM measured at 24 hrs post infection by focus forming assay | 2017 | ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3
| Structure-Activity Relationship Study of QL47: A Broad-Spectrum Antiviral Agent. |
AID1553407 | Antiproliferative activity against human Ramos cells assessed as reduction in cell growth incubated for 48 hrs by MTS assay | 2019 | Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
| Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors. |
AID1499250 | Antiproliferative activity against human Pfeiffer cells after 72 hrs by CellTiter-Glo assay | | | |
AID1880543 | Antiproliferative activity against CRBN knockout human JeKo-1 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay | 2022 | Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
| Structural Feature Analyzation Strategies toward Discovery of Orally Bioavailable PROTACs of Bruton's Tyrosine Kinase for the Treatment of Lymphoma. |
AID1469922 | Cell cycle arrest in human U2932 cells assessed as increase in accumulation at G0/G1 phase at 10 uM after 48 hrs by propidium iodide/RNase staining based flow cytometric method | | | |
AID1468809 | Inhibition of recombinant human cytoplasmic GST-tagged ERBB4 expressed in baculovirus at 1 uM by Z'-LYTE assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
| Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development. |
AID1469899 | Growth inhibition of human Ramos cells | | | |
AID1571259 | Cell cycle arrest in human Ramos cells assessed as apoptotic cells at 5 uM after 48 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 5.03%) | | | |
AID1738570 | Inhibition of BLK (unknown origin) by ADP-Glo assay | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold. |
AID1725090 | Half life in BALB/c mouse at 1 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery and Evaluation of Pyrazolo[3,4- |
AID1656238 | Inhibition of recombinant human BTK using fluoresceinated peptide as substrate after 60 mins fluorescence assay | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
| Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK). |
AID1851528 | Antiproliferative activity against human DOHH-2 cells incubated for 72 hrs by CellTiter-Glo assay | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Design, synthesis, and biological evaluation of pyrrolopyrimidine derivatives as novel Bruton's tyrosine kinase (BTK) inhibitors. |
AID1424893 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425192 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425054 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424969 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424981 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1738563 | Induction of cell cycle arrest in human Ramos cells assessed as subG1 phase accumulation at 5 uM incubated for 24 hrs by PI staining based flow cytometry analysis (Rvb = 2.53 %) | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold. |
AID1424946 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424972 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425080 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424894 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424941 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1772884 | Antiproliferative activity against human SNB-75 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors. |
AID1425108 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1401319 | Induction of apoptosis in human Ramos cells assessed as early apoptotic cells at 10 uM after 72 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.0%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma. |
AID1425068 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425211 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1458987 | Apparent permeability across basolateral to apical side in human Caco2 cells at 5 uM incubated for 2 hrs | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1738571 | Inhibition of SRC (unknown origin) by ADP-Glo assay | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold. |
AID1401330 | Induction of apoptosis in human Ramos cells assessed as total apoptosis rate at 10 uM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry relative to control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma. |
AID1418281 | Volume of distribution at steady state in mouse at 0.5 mg/kg, po | 2018 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
| Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk. |
AID1465439 | Inhibition of human TEC using poly[Glu:Tyr] as substrate preincubated for 20 mins followed by [gamma-33P]-ATP addition by filter binding method | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| In Silico Identification of a Novel Hinge-Binding Scaffold for Kinase Inhibitor Discovery. |
AID1822773 | Induction of cell cycle arrest in human U-937 cells assessed a accumulation of cells at G1 phase at 5 uM measured after 48 hrs by PI staining based flow cytometry analysis relative to control (Rvb = 51.40 %) | | | |
AID1397250 | Inhibition of BTK phosphorylation in human NAMALWA cells at 10 uM after 48 hrs by Western blot method | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
| Novel amino acid-substituted diphenylpyrimidine derivatives as potent BTK inhibitors against B cell lymphoma cell lines. |
AID1615366 | Inhibition of HER2 (unknown origin) preincubated for 1 hr followed by Biotin-AVLESEEELYSSARQ-NH2 substrate addition in presence of ATP and measured after 1 hr by TR-FRET assay | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1499241 | Antiproliferative activity against human A549 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1499237 | Inhibition of TEL-fused JAK3 (unknown origin) expressed in mouse BA/F3 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1553435 | Inhibition of BTK in anti-IgM-stimulated human Ramos cells assessed as reduction in autophosphorylation at Y223 residue at 10 uM incubated for 4 hrs followed by anti-IgM stimulation for 30 mins by Western blot analysis | 2019 | Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
| Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors. |
AID1425107 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425190 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1484554 | Antiproliferative activity against human Ramos cells over expressing BTK after 48 hrs by CCK-8 assay | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design and synthesis of sulfonamide-substituted diphenylpyrimidines (SFA-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B-cell lymphoblastic leukemia. |
AID1425076 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425091 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425210 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1714773 | Inhibition of BTK (unknown origin) at 0.1 uM by caliper mobility shift assay relative to control | | | |
AID1725082 | Inhibition of human ERG expressed in CHO cells at holding potential of -80 mV by patch clamp method | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery and Evaluation of Pyrazolo[3,4- |
AID1425069 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1334898 | Induction of apoptosis in human Ramos cells assessed as late apoptotic cells at 10 uM measured after 48 hrs by Annexin V-FITC/propidium iodide based flow cytometry relative to control | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
| Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines. |
AID1571254 | Induction of apoptosis in human Ramos cells assessed as late apoptotic cells at 5 uM after 48 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 0.98%) | | | |
AID1424948 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1399789 | Inhibition of BTK in whole blood (unknown origin) | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
| Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit. |
AID1155519 | Cytotoxicity against human DOHH2 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity. |
AID1245614 | Inhibition of BTK (unknown origin) after 1 hr by TR-FRET assay | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
| Synthesis and biological evaluation of novel 7-substituted 3-(4-phenoxyphenyl)thieno[3,2-c]pyridin-4-amines as potent Bruton's tyrosine kinase (BTK) inhibitors. |
AID1469888 | Inhibition of full length recombinant human N-terminal GST-tagged BMX expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 60 mins followed by substrate addition after 1 hr by ADP-Glo luminescence assay | | | |
AID1425000 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1375519 | Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
AID1897142 | Inhibition of recombinant wild-type BTK (unknown origin) assessed as inhibition of substrate phosphorylation using peptide substrate in presence of ATP by microplate reader assay | 2022 | RSC medicinal chemistry, Nov-16, Volume: 13, Issue:11
| Pyrazole-containing pharmaceuticals: target, pharmacological activity, and their SAR studies. |
AID1563053 | Induction of apoptosis in human Raji cells assessed as viable cells at 5 uM measured after 15 mins by Annexin-V-APC staining-based flow cytometric analysis (Rvb = 97.5 %) | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines. |
AID1714835 | Inhibition of ITK (unknown origin) | | | |
AID1424927 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1398715 | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
| Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3Kδ. |
AID1563055 | Induction of apoptosis in human Raji cells assessed as late apoptotic cells at 5 uM measured after 15 mins by Annexin-V-APC staining-based flow cytometric analysis (Rvb = 0.57 %) | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines. |
AID1426147 | Induction of apoptosis in human Ramos cells assessed as necrotic cells at 10 uM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1%) | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines. |
AID1468808 | Inhibition of recombinant human cytoplasmic GST-tagged LTK expressed in baculovirus at 1 uM by Z'-LYTE assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
| Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development. |
AID1475899 | Antiproliferative activity against human Mino cells at 25 uM preincubated for 48 hrs followed by thymidine addition measure after 16 hrs by Thymidine incorporation assay | 2017 | Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
| Anchimerically Activated ProTides as Inhibitors of Cap-Dependent Translation and Inducers of Chemosensitization in Mantle Cell Lymphoma. |
AID1772875 | Antiproliferative activity against human HCC 2998 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors. |
AID1469895 | Ratio of Kinact to Ki for full length recombinant human N-terminal His tagged BKT expressed in baculovirus infected Sf9 insect cells | | | |
AID1499233 | Inhibition of TEL-fused EGFR T790M/L858R mutant (unknown origin) expressed in mouse BA/F3 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1304229 | Irreversible inhibition of recombinant BTK (unknown origin) incubated for 1 hr by FRET assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Structure-based discovery of novel 4,5,6-trisubstituted pyrimidines as potent covalent Bruton's tyrosine kinase inhibitors. |
AID1375539 | Irreversible inhibition of BTK autophosphorylation at Y223 in human TMD8 cells at 1 uM preincubated for 2 hrs followed by compound wash out measured after 2 to 24 hrs by Western blot method | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
AID1424905 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1398717 | Inhibition of recombinant full length human N-terminal His tagged BTK expressed in baculovirus infected Sf9 cells at 200 nM using poly (4:1 Glu, Tyr) as substrate after 60 mins by ADP-Glo assay relative to control | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
| Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3Kδ. |
AID1398718 | Inhibition of recombinant full length human N-terminal His tagged BTK expressed in baculovirus infected Sf9 cells using poly (4:1 Glu, Tyr) as substrate after 60 mins by ADP-Glo assay | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
| Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3Kδ. |
AID1424965 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1334879 | Antiproliferative activity against human Raji cells measured after 48 hrs by CCK-8 assay | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
| Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines. |
AID1425182 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424907 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1560827 | Binding affinity to DNA-tagged recombinant ERBB2 (unknown origin) measured after 1 hr by biotinylated-ligand affinity bead-based qPCR analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1425059 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1267792 | Inhibition of FLT3 ITD mutant (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay | 2015 | Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
| Discovery of (R)-1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)-2-(dimethylamino)ethanone (CHMFL-FLT3-122) as a Potent and Orally Available FLT3 Kinase Inhibitor for FLT3-ITD Positive Acute Myeloid Leukemia. |
AID1424944 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1499229 | Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1401340 | Inhibition of JAK3 in human NAMALWA cells assessed as reduction in STAT3 phosphorylation at 10 uM after 48 hrs by immunoblot analysis | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma. |
AID1418295 | Intrinsic clearance in mouse microsomes | 2018 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
| Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk. |
AID1337177 | Inhibition of PF-06658607 binding to recombinant C-terminal FLAG-tagged FAM213A (unknown origin) expressed in HEK293T cells after 1 hr by gel-based ABPP assay | 2017 | Nature reviews. Drug discovery, Jun, Volume: 16, Issue:6
| Non-kinase targets of protein kinase inhibitors. |
AID1468849 | Inhibition of BTK C481S mutant (unknown origin) autophosphorylation at Y223 expressed in HEK293 cells at 1 uM by Western blot analysis | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
| Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development. |
AID1476268 | Antiproliferative activity against mouse BAF3 cells after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
AID1399790 | Fraction unbound in human plasma | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
| Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit. |
AID1375489 | Tmax in rat at 3 mg/kg, po | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
AID1425181 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1549566 | Inhibition of HER4 (unknown origin) | 2019 | European journal of medicinal chemistry, May-01, Volume: 169 | Design, synthesis and evaluation of novel 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as potent, selective and reversible Bruton's tyrosine kinase (BTK) inhibitors for the treatment of rheumatoid arthritis. |
AID1563038 | Induction of apoptosis in human Ramos cells assessed as early apoptotic cells at 5 uM measured after 15 mins by Annexin-V-APC staining-based flow cytometric analysis (Rvb = 0.14 %) | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines. |
AID1571258 | Cell cycle arrest in human Ramos cells assessed as accumulation of cells at G2/M phase at 5 uM after 48 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 4.26%) | | | |
AID1623569 | Inhibition of BTK in anti-human IgM-stimulated human Ramos cells assessed as reduction in BTK phosphorylation at Tyr223 residues after 4 hrs by Western blot analysis | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ. |
AID1880544 | Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay | 2022 | Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
| Structural Feature Analyzation Strategies toward Discovery of Orally Bioavailable PROTACs of Bruton's Tyrosine Kinase for the Treatment of Lymphoma. |
AID1267791 | Antiproliferative activity against human MV4-11 cells after 72 hrs by CelltiterGlo assay | 2015 | Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
| Discovery of (R)-1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)-2-(dimethylamino)ethanone (CHMFL-FLT3-122) as a Potent and Orally Available FLT3 Kinase Inhibitor for FLT3-ITD Positive Acute Myeloid Leukemia. |
AID1527027 | Growth inhibition of human OCI-LY10 cells at 42 nM incubated for 3 days by Alamar blue dye based fluorescence assay (Rvb = 3%) | | | |
AID1324665 | Cell cycle arrest in human Ramos cells assessed as accumulation at G2/M phase at 10 uM by propidium iodide staining based flow cytometry (Rvb = 1.58%) | 2016 | ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
| Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing a |
AID1878121 | Binding affinity to TEC (unknown origin) assessed as dissociation constant by KINOMEscan analysis | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors. |
AID1424955 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1615375 | Selectivity ratio of IC50 for ITK (unknown origin) to IC50 for N-terminal His-tagged recombinant human BTK (393 to 659 residues) expressed in baculovirus infected Sf9 cells | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1725074 | Protein binding in human plasma at 2 uM incubated for 4 hrs by LC-MS/MS analysis | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery and Evaluation of Pyrazolo[3,4- |
AID1484562 | Induction of apoptosis in human Ramos cells assessed as late apoptotic cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric analysis relative to control | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design and synthesis of sulfonamide-substituted diphenylpyrimidines (SFA-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B-cell lymphoblastic leukemia. |
AID1822805 | Inhibition of ITK in human Jurkat cells assessed as reduction in PLCgamma1 phosphorylation at 1000 nM incubated for 4 hrs by Western blot analysis | | | |
AID1725093 | AUC (0 to last) in BALB/c mouse at 1 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery and Evaluation of Pyrazolo[3,4- |
AID1560826 | Binding affinity to DNA-tagged recombinant EGFR (unknown origin) measured after 1 hr by biotinylated-ligand affinity bead-based qPCR analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1563075 | Inhibition of BTK in human Ramos cells assessed as reduction in PLCgamma-2 phosphorylation at Y1217 residue at 0.1 to 5 uM after 48 hrs by Western blot analysis | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines. |
AID1878130 | Selectivity index, ratio of Kd for TXK (unknown origin) to Kd for BTK (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors. |
AID1714855 | Inhibition of MEK2 (unknown origin) | | | |
AID1375491 | Oral bioavailability in rat at 3 mg/kg | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
AID1563076 | Inhibition of BTK in human Raji cells assessed as reduction in PLCgamma-2 phosphorylation at Y1217 residue at 0.1 to 5 uM after 48 hrs by Western blot analysis | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines. |
AID1878128 | Selectivity index, ratio of Kd for JAK3 (unknown origin) to Kd for BTK (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors. |
AID1324655 | Antiproliferative activity against human Ramos cells after 48 hrs by CCK-8 assay | 2016 | ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
| Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing a |
AID1458989 | Metabolic stability in human plasma at 5 uM incubated for 1 hr by LC-MS method | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1424914 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1401310 | Antiproliferative activity against human Raji cells after 72 hrs by CCK-8 assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma. |
AID1872689 | Cytotoxicity against human DOHH-2 cells expressing BTK and PI3kdelta assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Recent development of BTK-based dual inhibitors in the treatment of cancers. |
AID1424975 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1375559 | Antitumor activity against human TMD8 cells xenografted in CB17 SCID nude mouse assessed as effect on tumor volume at 25 mg/kg, po qd administered for 13 consecutive days measured on day 17 relative to control | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
AID1638808 | Intrinsic clearance in human liver microsomes at 3 uM measured up to 60 mins by LC/MS analysis | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors. |
AID1375530 | Inhibition of recombinant human ErbB2 using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
AID1481353 | Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1424982 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425056 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1469910 | Effect on BTK transphosphorylation at PLCgamma2 Y759 in human U2932 cells up to 1 uM measured after 4 hrs by chemiluminescent assay | | | |
AID631101 | Inhibition of LYN-A expressed in Sf9 cells after 60 mins by TR-FRET Assay | 2011 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
| Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis. |
AID1772874 | Antiproliferative activity against human NCI-H522 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors. |
AID1425067 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1469921 | Cell cycle arrest in human Pfeiffer cells assessed as increase in accumulation at G0/G1 phase at 10 uM after 48 hrs by propidium iodide/RNase staining based flow cytometric method | | | |
AID1869999 | Induction of cell cycle arrest in human SU-DHL-6 cells assessed as accumulation of cells at G0/G1 phase at 0.5 uM incubated for 24 hrs by PI staining based FACScan flow cytometry analysis (Rvb = 55.61 %) | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
| Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
AID1714819 | Antiarthritic activity in DBA/1J mouse model of collagen-induced arthritis at 20 mg/kg, po administered for 30 days and measured on day 30 | | | |
AID1560825 | Binding affinity to DNA-tagged recombinant ITK (unknown origin) measured after 1 hr by biotinylated-ligand affinity bead-based qPCR analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1880540 | Antiproliferative activity against human OCILY10 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay | 2022 | Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
| Structural Feature Analyzation Strategies toward Discovery of Orally Bioavailable PROTACs of Bruton's Tyrosine Kinase for the Treatment of Lymphoma. |
AID1822769 | Inhibition of EGFR phosphorylation in human A549 cells incubated for 4 hrs by Western blot assay | | | |
AID1412710 | Inhibition of human ErbB2 using using poly (4:1 Glu, Tyr) as substrate measured after 1 hr in presence of [gamma-33P]ATP | 2018 | MedChemComm, Apr-01, Volume: 9, Issue:4
| Discovery and biological evaluation of N5-substituted 6,7-dioxo-6,7-dihydropteridine derivatives as potent Bruton's tyrosine kinase inhibitors. |
AID1673830 | Inhibition of BMX (unknown origin) | 2019 | ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
| Design of Potent and Selective Covalent Inhibitors of Bruton's Tyrosine Kinase Targeting an Inactive Conformation. |
AID1638787 | Inhibition of wild type EGFR (unknown origin) by HTRF assay | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors. |
AID1673924 | Inhibition of wild type BTK (unknown origin) | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19
| Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations. |
AID1615386 | Selectivity ratio of IC50 for human TXK to IC50 for N-terminal His-tagged recombinant human BTK (393 to 659 residues) expressed in baculovirus infected Sf9 cells | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1164542 | Inhibition of cell proliferation of human Rec1 cells at 5 uM after 24 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | 4-Amino-2-arylamino-6-(2,6-dichlorophenyl)-pyrido[2,3-d]pyrimidin-7-(8H)-ones as BCR kinase inhibitors for B lymphoid malignancies. |
AID1425183 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425016 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1714870 | Inhibition of recombinant human FYN using biotinyl-beta Abeta-Abeta AYQAEENTYDEYEN as substrate incubate for 60 mins by LANCE assay | | | |
AID1870023 | Induction of apoptosis in human DOHH-2 cells assessed as early apoptotic cells at 1 uM incubated for 48 hrs by annexin V-FITC and PI staining based flow cytometry analysis (Rvb = 2.09 %) | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
| Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
AID1375531 | Inhibition of recombinant human FLT3 using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
AID1472050 | Growth inhibition of human SUDHL2 cells at 0.003 uM after 3 days by AlamarBlue assay (Rvb = - 1 %) | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
| Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88 |
AID1418289 | Inhibition of CYP2C8 (unknown origin) | 2018 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
| Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk. |
AID1425106 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1714850 | Inhibition of CSK (unknown origin) | | | |
AID1656236 | Inhibition of BTK in human whole blood cells after 1 hr by ELISA | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
| Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK). |
AID1720538 | Inhibition of recombinant full length human His-tagged BLK cytoplasmic domain expressed in baculovirus expression system using tyrosine-1 peptide as substrate preincubated for 1 hr in presence of ATP by Z'-LYTE assay | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
| Discovery of quinoline-based irreversible BTK inhibitors. |
AID1830231 | Inhibition of BTK in human Ramos cells assessed as reduction in BTK phosphorylation at Tyr223 residue incubated for 24 hrs by Western blot analysis | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
| Discovery of AS-1763: A Potent, Selective, Noncovalent, and Orally Available Inhibitor of Bruton's Tyrosine Kinase. |
AID1623559 | Antiproliferative activity against human Raji cells at 5 uM after 24 hrs by CCK8 assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ. |
AID1574157 | Antiproliferative activity against human SU-DHL6 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
| Synthesis and biological evaluation of novel 1-substituted 3-(3-phenoxyprop-1-yn-1-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amines as potent Bruton's tyrosine kinase (BTK) inhibitors. |
AID1425127 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1615368 | Inhibition of human BMX using poly[Glu:Tyr] (4:1) as substrate preincubated for 60 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by filter binding method | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1458991 | Fraction unbound in mouse 100% plasma at 5 uM incubated for 6 hrs by LC-MS method | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1725080 | Inhibition of human liver microsome CYP2C9 using diclofenac as substrate preincubated for 10 mins followed by substrate and NADPH addition and measured after 10 mins by LC-MS/MS analysis | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery and Evaluation of Pyrazolo[3,4- |
AID1424979 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1499253 | Antiproliferative activity against human NALM6 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1499271 | Antiproliferative activity against primary CLL cells derived from p12 patient after 72 hrs by CellTiter-Glo assay | | | |
AID1425057 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1571252 | Induction of apoptosis in human Ramos cells assessed as viable cells at 5 uM after 48 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 96.83%) | | | |
AID1469911 | Inhibition of BTK transphosphorylation at PLCgamma2 Y1217 in human U2932 cells up to 1 uM measured after 4 hrs by chemiluminescent assay | | | |
AID1714868 | Inhibition of HCK (unknown origin) | | | |
AID1638801 | Apparent permeability across basolateral to apical side in human Caco2 cells at 5 uM after 2 hrs by transwell membrane based assay | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors. |
AID1425042 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425104 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425196 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1615372 | Inhibition of human FRK using poly[Glu:Tyr] (4:1) as substrate preincubated for 60 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by filter binding method | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1164541 | Inhibition of BTK phosphorylation in human Rec1 cells at 2.5 uM incubated for 6 hrs by Western blotting method | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | 4-Amino-2-arylamino-6-(2,6-dichlorophenyl)-pyrido[2,3-d]pyrimidin-7-(8H)-ones as BCR kinase inhibitors for B lymphoid malignancies. |
AID1571255 | Induction of apoptosis in human Ramos cells assessed as necrotic cells at 5 uM after 48 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 1.11%) | | | |
AID1425063 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1399782 | Inhibition of human full length BTK using FITC-AHA-EEPLYWSFPAKKK-NH2 as substrate after 90 mins by microfluid mobility shift assay | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
| Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit. |
AID1397247 | Induction of apoptosis in human NAMALWA cells assessed as late apoptotic cells at 5 uM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0%) | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
| Novel amino acid-substituted diphenylpyrimidine derivatives as potent BTK inhibitors against B cell lymphoma cell lines. |
AID1870013 | Induction of cell cycle arrest in human DOHH-2 cells assessed as accumulation of cells at G2/M phase at 1 uM incubated for 24 hrs by PI staining based flow cytometry analysis (Rvb = 21.42 %) | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
| Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
AID1725075 | Protein binding in rat plasma at 2 uM incubated for 4 hrs by LC-MS/MS analysis | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery and Evaluation of Pyrazolo[3,4- |
AID1484553 | Inhibition of human recombinant full-length N-terminal His-tagged BTK expressed in baculovirus infected Sf9 insect cells after 60 mins by ADP-Glo kinase assay | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design and synthesis of sulfonamide-substituted diphenylpyrimidines (SFA-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B-cell lymphoblastic leukemia. |
AID1638788 | Inhibition of EGFR L858R/T790M double mutant (unknown origin) by HTRF assay | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors. |
AID1424889 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1725089 | Oral bioavailability in Sprague-Dawley rat at 10 mg/kg measured upto 24 hrs by LC-MS/MS analysis | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery and Evaluation of Pyrazolo[3,4- |
AID1878117 | Binding affinity to BTK (unknown origin) assessed as dissociation constant by KINOMEscan analysis | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors. |
AID1720522 | Inhibition of His-tagged recombinant human TEC expressed in baculovirus expression system preincubated for 1 hr by Z'lyte assay | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
| Discovery of quinoline-based irreversible BTK inhibitors. |
AID1475902 | Inhibition of eIF4E in human Mino cells assessed as down regulation of c-Myc protein expression at 10 to 25 uM after 48 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
| Anchimerically Activated ProTides as Inhibitors of Cap-Dependent Translation and Inducers of Chemosensitization in Mantle Cell Lymphoma. |
AID1560882 | Inhibition of BTK in human basophils assessed as reduction in anti-IgE mouse IgG1 antibody Le2-stimulated CD63 expression on basophil preincubated for 30 mins in presence of IgE antibody B11 followed by anti-IgE mouse IgG1 antibody Le2 stimulation and mea | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1397234 | Antiproliferative activity against human NAMALWA cells after 72 hrs by CCK8 assay | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
| Novel amino acid-substituted diphenylpyrimidine derivatives as potent BTK inhibitors against B cell lymphoma cell lines. |
AID1425099 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1714881 | Inhibition of recombinant human PI3K using PIP2 as substrate incubate for 15 mins by LANCE assay | | | |
AID1870017 | Induction of apoptosis in human SU-DHL-6 cells assessed as necrotic cells at 1.5 uM incubated for 48 hrs by annexin V-FITC and PI staining based flow cytometry analysis (Rvb = 0.32%) | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
| Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
AID1563025 | Inhibition of human recombinant full length N-terminal His tagged BTK C481S mutant expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate measured after 60 mins in presence of ATP by ADP-Glo kinase assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines. |
AID1563022 | Antiproliferative activity against human Ramos cells measured after 72 hrs by CCK-8 assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines. |
AID1623573 | Cell cycle arrest in human Ramos cells assessed as accumulation at apoptotic phase at 5 uM after 48 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 5.03%) | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ. |
AID1458993 | Intrinsic clearance in human liver microsomes at 3 uM after 50 mins by LC-MS method | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1499231 | Inhibition of TEL-fused EGFR T790M mutant (unknown origin) expressed in mouse BA/F3 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1399788 | Inhibition of BTK in human PBMC assessed as reduction in anti-IgM-induced CD69 expression incubated for 1 hr by flow cytometric analysis | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
| Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit. |
AID1164540 | Inhibition of Lyn phosphorylation in human Rec1 cells at 2.5 uM incubated for 6 hrs by Western blotting method | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | 4-Amino-2-arylamino-6-(2,6-dichlorophenyl)-pyrido[2,3-d]pyrimidin-7-(8H)-ones as BCR kinase inhibitors for B lymphoid malignancies. |
AID1615365 | Inhibition of TEC (unknown origin) preincubated for 1 hr followed by Biotin-AVLESEEELYSSARQ-NH2 substrate addition in presence of ATP and measured after 1 hr by TR-FRET assay | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1458984 | Selectivity ratio of EC50 for human A431 cells expressing wild type EGFR to EC50 for human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1714856 | Inhibition of RET (unknown origin) | | | |
AID1878129 | Selectivity index, ratio of Kd for TEC (unknown origin) to Kd for BTK (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors. |
AID1425033 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1469904 | Growth inhibition of human SKM1 cells | | | |
AID1375525 | Inhibition of recombinant human EGFR using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
AID1638803 | Apparent permeability across basolateral to apical side in MDCK2-MDR1 cells at 10 uM after 2 hrs by transwell membrane based assay | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors. |
AID1425004 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425061 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425213 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1615391 | Selectivity ratio of IC50 for ITK in human Jurkat cells to IC50 for BTK in human Ramos cells | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1425089 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1673835 | Irreversible inhibition of full length human unphosphorylated BTK at 5.7 uM using peptide substrate preincubated for 2 hrs followed by compound dilution and measured after substrate addition for 1 hr in presence of ATP at Km concentration | 2019 | ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
| Design of Potent and Selective Covalent Inhibitors of Bruton's Tyrosine Kinase Targeting an Inactive Conformation. |
AID1650930 | Inhibition of BTK (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 30, Issue:3
| Design, synthesis and biological evaluation of Proteolysis Targeting Chimeras (PROTACs) as a BTK degraders with improved pharmacokinetic properties. |
AID1458990 | Metabolic stability in mouse plasma at 5 uM incubated for 1 hr by LC-MS method | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1375527 | Inhibition of recombinant human TXK using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
AID1650544 | Inhibition of recombinant human N-terminal His-tagged JAK3 (795 to 1124 residues) expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay | 2020 | Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
| Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors. |
AID1401308 | Inhibition of recombinant N-terminal GST-tagged human JAK3 (781 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly(4:1 Glu,Tyr) peptide substrate incubated for 60 mins by ADP-Glo luminescence assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma. |
AID1851526 | Antiproliferative activity against human OCILY3 cells incubated for 72 hrs by CellTiter-Glo assay | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Design, synthesis, and biological evaluation of pyrrolopyrimidine derivatives as novel Bruton's tyrosine kinase (BTK) inhibitors. |
AID1417598 | Efflux ratio of permeability in human Caco2 cells | 2018 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20
| Optimization of the efflux ratio and permeability of covalent irreversible BTK inhibitors. |
AID1424954 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1481308 | Inhibition of EGFR L858R mutant in human H3255 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1563060 | Cell cycle arrest in human Ramos cells assessed as accumulation at G0/G1 phase at 1 uM measured after 48 hrs by propidium iodide/RNase staining based flow cytometric analysis (Rvb = 37.66 %) | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines. |
AID1425151 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425008 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1375533 | Inhibition of recombinant human PDGFR-beta using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
AID1458985 | Permeability of the compound at 500 uM incubated for 20 hrs by PAMPA | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1650555 | Metabolic stability in human liver microsomes assessed as intrinsic clearance at 0.2 uM incubated for 60 mins by UPLC-MS/MS analysis | 2020 | Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
| Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors. |
AID1878116 | Binding affinity to BMX (unknown origin) assessed as dissociation constant by KINOMEscan analysis | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors. |
AID1524892 | Stability in human liver microsomes assessed as compound remaining incubated of 60 mins in presence of NADPH regenerating system by LC/MS analysis | 2019 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
| Discovery of novel pyrazole derivatives as potential anticancer agents in MCL. |
AID1155521 | Cytotoxicity against human SU-DHL6 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity. |
AID1424926 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424991 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425066 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1499242 | Antiproliferative activity against human NCI-H358 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1418287 | Inhibition of CYP2B6 (unknown origin) | 2018 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
| Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk. |
AID1623562 | Induction of apoptosis in human Ramos cells assessed as early apoptotic cells at 5 uM after 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometric analysis (Rvb = 1.08%) | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ. |
AID1894185 | Inhibition of ERK phosphorylation in anti-IgG stimulated human DOHH-2 cells preincubated for 1 hr followed by compound washout and anti-IgG stimulation for 2 mins by chemiluminescence based Western blotting analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application. |
AID1871762 | Inhibition of ITK (unknown origin) | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Review of the development of BTK inhibitors in overcoming the clinical limitations of ibrutinib. |
AID1560822 | Binding affinity to DNA-tagged recombinant BTK (unknown origin) measured after 1 hr by biotinylated-ligand affinity bead-based qPCR analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1878115 | Binding affinity to BLK (unknown origin) assessed as dissociation constant by KINOMEscan analysis | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors. |
AID1725084 | Clearance in Sprague-Dawley rat at 2 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery and Evaluation of Pyrazolo[3,4- |
AID1574158 | Antiproliferative activity against human WSU-DLCL2 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
| Synthesis and biological evaluation of novel 1-substituted 3-(3-phenoxyprop-1-yn-1-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amines as potent Bruton's tyrosine kinase (BTK) inhibitors. |
AID1894182 | Inhibition of BTK in human DOHH-2 cells preincubated for 1 hr followed by compound washout and anti-IgG stimulation for 2 mins by chemiluminescence based Western blotting analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application. |
AID1425166 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424931 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424901 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1615374 | Inhibition of human TXK using poly[Glu:Tyr] (4:1) as substrate preincubated for 60 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by filter binding method | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1424976 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425074 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1876107 | Cytotoxicity against human PC-3 cells | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
AID1615385 | Selectivity ratio of IC50 for human LCK to IC50 for N-terminal His-tagged recombinant human BTK (393 to 659 residues) expressed in baculovirus infected Sf9 cells | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1425096 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1738560 | Induction of cell cycle arrest in human Ramos cells assessed as G0/G1 phase accumulation at 5 uM incubated for 24 hrs by PI staining based flow cytometry analysis (Rvb = 39.13 %) | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold. |
AID1889496 | Inhibition of BTK (unknown origin) by lanthascreen Tb kinase activity assay | 2022 | Journal of natural products, 02-25, Volume: 85, Issue:2
| Ophiorrhines F and G, Key Biogenetic Intermediates of Ophiorrhine Alkaloids from |
AID1484563 | Induction of apoptosis in human Ramos cells assessed as necrotic cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 0.2%) | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design and synthesis of sulfonamide-substituted diphenylpyrimidines (SFA-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B-cell lymphoblastic leukemia. |
AID1656245 | Inhibition of His-tagged BTK (unknown origin) assessed as ratio of Kinact to Ki(app) after 1.5 hrs by HTRF analysis | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
| Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK). |
AID1375485 | Clearance in rat at 1 mg/kg, iv | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
AID1488735 | Aqueous solubility of the compound at 1 mg | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
| Discovery of (R)-5-(benzo[d][1,3]dioxol-5-yl)-7-((1-(vinylsulfonyl)pyrrolidin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (B6) as a potent Bmx inhibitor for the treatment of NSCLC. |
AID1425060 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1615445 | Oral bioavailability in human in fed state at 560 mg administered daily | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1488740 | Antitumor activity against human NCI-H1975 cells xenografted in nude mouse assessed as tumor growth inhibition at 25 mg/kg administered via oral gavage qd measured every 2 days up to 18 days relative to control | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
| Discovery of (R)-5-(benzo[d][1,3]dioxol-5-yl)-7-((1-(vinylsulfonyl)pyrrolidin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (B6) as a potent Bmx inhibitor for the treatment of NSCLC. |
AID1425111 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1499232 | Inhibition of TEL-fused EGFR L858R mutant (unknown origin) expressed in mouse BA/F3 cells after 72 hrs by CellTiter-Glo assay | | | |
AID1309835 | Cytotoxicity against human MIAPaCa2 cells assessed as cell growth inhibition after 3 days by presto blue dye based plate reader method | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Isatin Derived Spirocyclic Analogues with α-Methylene-γ-butyrolactone as Anticancer Agents: A Structure-Activity Relationship Study. |
AID1424918 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1574152 | Inhibition of recombinant full-length human N-terminal GST-fused BTK (2 to 659 residues) expressed in baculovirus expression system using biotin-labelled peptide as substrate measured after 50 mins by TR-FRET assay | 2019 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
| Synthesis and biological evaluation of novel 1-substituted 3-(3-phenoxyprop-1-yn-1-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amines as potent Bruton's tyrosine kinase (BTK) inhibitors. |
AID1424985 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1714772 | Inhibition of BTK (unknown origin) at 1 uM by caliper mobility shift assay relative to control | | | |
AID1714839 | Inhibition of ErBB2 (unknown origin) | | | |
AID1725092 | Volume of distribution at steady state in BALB/c mouse at 1 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery and Evaluation of Pyrazolo[3,4- |
AID1673819 | Terminal plasma concentration in ovalbumin-immunized C57Bl6 mouse at 30 mg/kg, po administered 2 h prior to OVA immunization and measured after 5 hrs | 2019 | ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
| Design of Potent and Selective Covalent Inhibitors of Bruton's Tyrosine Kinase Targeting an Inactive Conformation. |
AID1638786 | Inhibition of N-terminal His-tagged MKK7 beta1 S273D/T275D double mutant (unknown origin) expressed in insect cells using JNK1 K55M mutant as substrate by ADP-Glo assay | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors. |
AID1549595 | Antiarthritic activity in DBA1/J mouse model of collagen-induced arthritis assessed as reduction in cartilage damage at 12.5 mg/kg, po qd by H and E staining based assay | 2019 | European journal of medicinal chemistry, May-01, Volume: 169 | Design, synthesis and evaluation of novel 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as potent, selective and reversible Bruton's tyrosine kinase (BTK) inhibitors for the treatment of rheumatoid arthritis. |
AID1425136 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425120 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1527030 | Growth inhibition of human OCI-LY19 cells at 4.2 nM incubated for 3 days by Alamar blue dye based fluorescence assay (Rvb = 3%) | | | |
AID1549565 | Inhibition of human recombinant HER2 using biotinyl-beta amyloid beta amyloid beta AAEEEEYFELVAKKK measured after 10 mins in the presence of ATP by HTRF assay | 2019 | European journal of medicinal chemistry, May-01, Volume: 169 | Design, synthesis and evaluation of novel 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as potent, selective and reversible Bruton's tyrosine kinase (BTK) inhibitors for the treatment of rheumatoid arthritis. |
AID1709139 | Inhibition of BTK (unknown origin) One-hour enzymatic assay without pre-incubation | 2021 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 38 | Small molecule approaches to treat autoimmune and inflammatory diseases (Part I): Kinase inhibitors. |
AID1423320 | Glutathione reactivity assessed as formation of glutathione adduct formation in presence of pH 7.4 at 25 degC by NMR based method | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
| Neolymphostin A Is a Covalent Phosphoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitor That Employs an Unusual Electrophilic Vinylogous Ester. |
AID1425131 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1650551 | Antiproliferative activity against human HEL cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | 2020 | Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
| Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors. |
AID1870041 | Antitumor activity against human SU-DHL-6 cells xenografted in NOD/SCID mouse assessed as tumor volume suppression at 10 mg/kg, po qd measured every 2 days | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
| Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. |
AID1375480 | Inhibition of recombinant full-length N-terminal His-tagged human BTK C481S mutant expressed in baculovirus infected Sf9 insect cells using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
AID1650542 | Inhibition of recombinant human N-terminal GST-tagged JAK1 (850 to 1154 residues) expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay | 2020 | Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
| Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors. |
AID1418284 | Inhibition of human ERG | 2018 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
| Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk. |
AID1720509 | Inhibition of recombinant human GST-tagged EGFR (668 to 1210 residues) expressed in baculovirus expression system using Tyr 04 peptide as substrate preincubated for 1 hr by Z'-LYTE assay | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
| Discovery of quinoline-based irreversible BTK inhibitors. |
AID1720528 | Inhibition of recombinant human GST-tagged JAK3 catalytic domain (781 to 1124 residues) expressed in baculovirus expression system using tyrosine-6 peptide as substrate preincubated for 1 hr in presence of ATP by Z'-LYTE assay | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
| Discovery of quinoline-based irreversible BTK inhibitors. |
AID1458981 | Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1425141 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1563039 | Induction of apoptosis in human Ramos cells assessed as late apoptotic cells at 5 uM measured after 15 mins by Annexin-V-APC staining-based flow cytometric analysis (Rvb = 1.85 %) | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines. |
AID1527031 | Growth inhibition of human OCI-LY19 cells at 10 nM incubated for 3 days by Alamar blue dye based fluorescence assay (Rvb = 3%) | | | |
AID1623570 | Inhibition of BTK in anti-human IgM-stimulated human Ramos cells assessed as reduction in PLCgamma2 phosphorylation at Tyr1217 residues after 4 hrs by Western blot analysis | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ. |
AID1458977 | Inhibition of human recombinant GST-tagged EGFR L858R mutant expressed in baculovirus expression system preincubated for 30 mins followed by ATP and TK-substrate addition measured after 15 mins by HTRF assay | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1241390 | Inhibition of BTK (unknown origin) | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
| Discovery of thieno[3,2-c]pyridin-4-amines as novel Bruton's tyrosine kinase (BTK) inhibitors. |
AID1725085 | Volume of distribution at steady state in Sprague-Dawley rat at 2 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery and Evaluation of Pyrazolo[3,4- |
AID1458982 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1623549 | Inhibition of BTK (unknown origin) by ADP-gloassay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ. |
AID1587020 | Inhibition of full-length recombinant human C-terminal His-tagged SRC cytoplasmic domain expressed in baculovirus expression system using FAM-Srctide peptide as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr by TR-F | 2019 | ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
| Aminopyrazole Carboxamide Bruton's Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning. |
AID1738558 | Induction of apoptosis in human Ramos cells assessed as late apoptotic cells at 5 uM incubated for 24 hrs by annexin V-FITC and PI staining based flow cytometry analysis (Rvb = 2.2 %) | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold. |
AID1638812 | Covalent binding affinity to MKK7 (unknown origin) assessed as formation of covalent bond with Cys218 residues by MS/MS analysis | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors. |
AID1425157 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1615341 | Inhibition of JAK3 (unknown origin) preincubated for 1 hr followed by Biotin-AVLESEEELYSSARQ-NH2 substrate addition in presence of ATP and measured after 1 hr by TR-FRET assay | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1638809 | Intrinsic clearance in mouse liver microsomes at 3 uM measured up to 60 mins by LC/MS analysis | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors. |
AID1458986 | Apparent permeability across apical to basolateral side in human Caco2 cells at 5 uM incubated for 2 hrs | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1673834 | Inhibition of EGFR (unknown origin) | 2019 | ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
| Design of Potent and Selective Covalent Inhibitors of Bruton's Tyrosine Kinase Targeting an Inactive Conformation. |
AID1334886 | Cell cycle arrest in human Ramos cells assessed as accumulation at G0/G1 phase at 10 uM measured after 48 hrs by propidium iodide based flow cytometry (Rvb = 39.95 %) | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
| Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines. |
AID1615373 | Inhibition of human LCK using poly[Glu:Tyr] (4:1) as substrate preincubated for 60 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by filter binding method | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1425055 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1425078 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1782000 | Selectivity index, ratio of IC50 for inhibition of BMX (unknown origin) to IC50 for inhibition of BTK (unknown origin) | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
| Discovery of 1-Amino-1 |
AID1560834 | Selectivity ratio of Kd for DNA-tagged recombinant ERBB2 (unknown origin) to Kd for DNA-tagged recombinant BTK (unknown origin) | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1425138 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424912 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1851525 | Antiproliferative activity against human Pfeiffer cells incubated for 72 hrs by CellTiter-Glo assay | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Design, synthesis, and biological evaluation of pyrrolopyrimidine derivatives as novel Bruton's tyrosine kinase (BTK) inhibitors. |
AID1563071 | Cell cycle arrest in human Raji cells assessed as accumulation at G2/M phase at 1 uM measured after 48 hrs by propidium iodide/RNase staining based flow cytometric analysis (Rvb = 18.14 %) | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines. |
AID1871767 | Inhibition of ERBB4 (unknown origin) | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Review of the development of BTK inhibitors in overcoming the clinical limitations of ibrutinib. |
AID1615371 | Inhibition of human FGR using poly[Glu:Tyr] (4:1) as substrate preincubated for 60 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by filter binding method | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
AID1563019 | Inhibition of human recombinant full length N-terminal His tagged BTK expressed in baculovirus infected Sf9 cells at 10 uM using poly (Glu,Tyr) 4:1 as substrate measured after 60 mins in presence of ATP by ADP-Glo kinase assay relative to control | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines. |
AID1869073 | Inhibition of BTK T474M mutant (unknown origin) expressed in baculovirus infected Trichoplusia ni pro cells incubated for 30 mins in presence of ATP by Microfluidic chip based mobility shift assay | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
| Medicinal Chemistry Strategies for the Development of Bruton's Tyrosine Kinase Inhibitors against Resistance. |
AID1469897 | Growth inhibition of human MV411 cells | | | |
AID1424967 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1714834 | Inhibition of Tec (unknown origin) | | | |
AID1725095 | Antiarthritic activity in collagen-induced arthritis mouse model assessed as clinical score at 10 mg/kg, po administered for 14 days and measured for 21 days after dosing | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery and Evaluation of Pyrazolo[3,4- |
AID1425110 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1424952 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1822786 | Toxicity in human U-937 cells xenografted in BALB/c nude mouse assessed as increase in body weight at 25 mg/kg, po administered once daily 14 days | | | |
AID1412327 | Glutathione reactivity of the compound assessed as pseudo first order reaction rate constant for GSH adduct formation at 37 degC by LC analysis | | | |
AID1425093 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
AID1714873 | Inhibition of recombinant human SRC using Ulight-Poly GAT[EAY(1:1:1)]n as substrate incubate for 10 mins by LANCE assay | | | |
AID1347125 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
AID1347109 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
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. |
AID1347128 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347115 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
AID1347119 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
AID1347113 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347129 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
AID1347118 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347117 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1347110 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
AID1347127 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347112 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
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. |
AID1347111 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347116 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
AID1347121 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347114 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347124 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
AID1347123 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
AID1347122 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347126 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |