LY-2157299: an orally active transforming growth factor beta receptor (TGF-beraR) kinase inhibitor [MeSH]
LY-2157299 : A pyrrolopyrazole that is 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole which is substituted at positions 2 and 3 by 6-methylpyridin-2-yl and 6-(aminocarbonyl)quinolin-4-yl groups, respectively. A Transforming growth factor-betaRI (TGF-betaRI) kinase inhibitor, it blocks TGF-beta-mediated tumor growth in glioblastoma. [CHeBI]
| ID Source | ID |
|---|---|
| PubMed CID | 10090485 |
| CHEMBL ID | 2364611 |
| SCHEMBL ID | 12922153 |
| CHEBI ID | 137064 |
| MeSH ID | M0557245 |
| Synonym |
|---|
| 4-(2-(6-methylpyridin-2-yl)-5,6-dihydro-4h-pyrrolo[1,2-b]pyrazol-3-yl)quinoline-6-carboxamide |
| HY-13226 |
| CHEBI:137064 |
| galunisertibum |
| 700874-72-2 |
| ly-2157299 |
| ly 2157299 |
| galunisertib , |
| ly2157299 , |
| 4-[2-(6-methylpyridin-2-yl)-5,6-dihydro-4h-pyrrolo[1,2-b]pyrazol-3-yl]quinoline-6-carboxamide |
| A836766 |
| 4-[2-(6-methyl-2-pyridinyl)-5,6-dihydro-4h-pyrrolo[1,2-b]pyrazol-3-yl]-6-quinolinecarboxamide |
| EX-8675 |
| 4-(2-(6-methylpyridin-2-yl)-5,6-dihydro-4h-pyrrolo(1,2-b)pyrazol-3-yl)quinoline-6-carboxylic acid amide |
| unii-3okh1w5lze |
| 3okh1w5lze , |
| galunisertib [usan:inn] |
| 6-quinolinecarboxamide, 4-(5,6-dihydro-2-(6-methyl-2-pyridinyl)-4h-pyrrolo(1,2-b)pyrazol-3-yl)- |
| 4-[2-(6-methylpyridin-2-yl)-4h,5h,6h-pyrrolo[1,2-b]pyrazol-3-yl]quinoline-6-carboxamide |
| galunisertib (usan) |
| D10437 |
| CS-0474 |
| S2230 |
| 4-[5,6-dihydro-2-(6-methyl-2-pyridinyl)-4h-pyrrolo[1,2-b]pyrazol-3-yl]-6-quinolinecarboxamide |
| CHEMBL2364611 |
| inhibitor 15d [pmid: 18314943] |
| gtpl7797 |
| 4-[2-(6-methylpyridin-2-yl)-5,6-dihydro-4h-pyrrolo[2,1-e]pyrazol-3-yl]quinoline-6-carboxamide |
| AKOS022175280 |
| 6-quinolinecarboxamide, 4-(5,6-dihydro-2-(6-methyl-2-pyridinyl)-4h-pyrrolo(1,2-b)pyrazol-3-yl)-) |
| galunisertib [who-dd] |
| galunisertib [inn] |
| galunisertib [usan] |
| DTXSID00220362 |
| SCHEMBL12922153 |
| 4-[2-(6-methyl-pyridin-2-yl)-5,6-dihydro-4h-pyrrolo[1,2-b]pyrazol-3-yl]-quinoline-6-carboxylic acid amide |
| bdbm50015640 |
| AC-31327 |
| galunisertib (ly2157299) |
| J-514250 |
| mfcd12923319 |
| EX-A009 |
| 4-(2-(6-methylpyridin-2-yl)-5,6-dihydro-4h-pyrrolo[1,2-b]pyrazol-3-yl)quinoline-6-carboxamide, aldrichcpr |
| HMS3655D14 |
| NCGC00384167-07 |
| SW219460-1 |
| 4-(2-(6-methylpyridin-2-yl)-5,6-dihydro-4h-pyrrolo-[1,2-b]pyrazol-3-yl)quinoline-6-carboxamide |
| ly2157299(galunisertib) |
| DB11911 |
| FT-0741808 |
| AS-42940 |
| Q27077768 |
| BCP02173 |
| SB16483 |
| AMY9045 |
| CCG-264950 |
| nsc-800103 |
| nsc761216 |
| nsc-761216 |
| nsc800103 |
| Role | Description |
|---|---|
| TGFbeta receptor antagonist | An antagonist that binds to and deactivates TGFbeta receptors. |
| antineoplastic agent | A substance that inhibits or prevents the proliferation of neoplasms. |
| Class | Description |
|---|---|
| quinolines | A class of aromatic heterocyclic compounds each of which contains a benzene ring ortho fused to carbons 2 and 3 of a pyridine ring. |
| pyrrolopyrazole | |
| methylpyridines | Any member of the class of pyridines that carries at least one methyl substituent. |
| aromatic amide | An amide in which the amide linkage is bonded directly to an aromatic system. |
| monocarboxylic acid amide | A carboxamide derived from a monocarboxylic acid. |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
|---|---|---|---|---|
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 37.9083 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 37.9083 | AID1645842 |
| Interferon beta | Homo sapiens (human) | Potency | 37.9083 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 37.9083 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 37.9083 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 37.9083 | AID1645842 |
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 ISSN: 1554-8937 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425001 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424926 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425000 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425140 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425193 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1634302 | Inhibition of human recombinant untagged p38alpha expressed in Escherichia coli using ATF2 as substrate incubated for 60 mins in presence of [33P]-ATP by scintillation counting method | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 ISSN: 1464-3405 | Synthesis and biological evaluation of novel benzo[c][1,2,5]thiadiazol-5-yl and thieno[3,2-c]- pyridin-2-yl imidazole derivatives as ALK5 inhibitors. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424971 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425149 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424934 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425181 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425102 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1563857 | Inhibition of ALK5 in human LX2 cells assessed as reduction in TGFbeta-induced collagen 1 production at 5 uM pretreated for 1 hr followed by TGFbeta addition and measured after 12 hrs by DAPI staining based immunocytochemistry analysis by confocal laser s | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180ISSN: 1768-3254 | Design, synthesis, and antifibrosis evaluation of 4-(benzo-[c][1,2,5]thiadiazol-5-yl)-3(5)-(6-methyl- pyridin-2-yl)pyrazole and 3(5)-(6-methylpyridin- 2-yl)-4-(thieno-[3,2,-c]pyridin-2-yl)pyrazole derivatives. |
| AID1142660 | Inhibition of ALK5 in human HaCaT cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 ISSN: 1520-4804 | Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425150 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425199 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425058 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425176 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424928 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425136 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425156 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425057 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425186 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425022 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425059 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1733256 | Inhibition of epithelial-mesenchymal transition in human U-87MG cells assessed as reduction in TGF-beta stimulated Slug protein expression after 48 hrs by Western blot anlaysis | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216ISSN: 1768-3254 | Synthesis and evaluation of the epithelial-to- mesenchymal inhibitory activity of indazole-derived imidazoles as dual ALK5/p38α MAP inhibitors. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1653826 | Induction of apoptosis in human HCT116 cells assessed as late apoptotic cells at 50 uM after 12 hrs by Annexin-V/PI-staining based flow cytometric analysis (Rvb = 0.2%) | 2020 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2 ISSN: 1464-3405 | Synthesis and evaluation of the HIF-1α inhibitory activity of 3(5)-substituted-4-(quinolin-4-yl)- and 4-(2-phenylpyridin-4-yl)pyrazoles as inhibitors of ALK5. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1563858 | Inhibition of ALK5 in human LX2 cells assessed as reduction in TGFbeta-induced alphaSMA production at 5 uM pretreated for 1 hr followed by TGFbeta addition and measured after 12 hrs by DAPI staining based immunocytochemistry analysis by confocal laser sca | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180ISSN: 1768-3254 | Design, synthesis, and antifibrosis evaluation of 4-(benzo-[c][1,2,5]thiadiazol-5-yl)-3(5)-(6-methyl- pyridin-2-yl)pyrazole and 3(5)-(6-methylpyridin- 2-yl)-4-(thieno-[3,2,-c]pyridin-2-yl)pyrazole derivatives. |
| AID1423862 | Cytotoxicity against human K562 cells assessed as decrease in cell proliferation after 72 hrs by calcein AM staining-based assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127ISSN: 1768-3254 | ALK5 kinase inhibitory activity and synthesis of 2,3,4-substituted 5,5-dimethyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazoles. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425027 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424917 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424999 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1653821 | Inhibition of TNFalpha-induced HIF1alpha expression in human HCT116 cells at 50 uM by Western blot analysis | 2020 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2 ISSN: 1464-3405 | Synthesis and evaluation of the HIF-1α inhibitory activity of 3(5)-substituted-4-(quinolin-4-yl)- and 4-(2-phenylpyridin-4-yl)pyrazoles as inhibitors of ALK5. |
| AID1733260 | Reversal of TGF-beta-induced epithelial-mesenchymal transition in human U-87MG cells assessed as reduction in N-cadherin protein level at 0.1 to 0.5 uM after 48 hrs by Western blotting analysis | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216ISSN: 1768-3254 | Synthesis and evaluation of the epithelial-to- mesenchymal inhibitory activity of indazole-derived imidazoles as dual ALK5/p38α MAP inhibitors. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425020 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424973 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424935 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424944 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425021 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424977 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1772983 | Inhibition of TGFBR1 (unknown origin) at 20 uM relative to control | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223ISSN: 1768-3254 | Discovery and biological evaluation of phthalazines as novel non-kinase TGFβ pathway inhibitors. |
| AID1425178 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424954 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425004 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425172 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425194 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1653812 | Inhibition of recombinant human p38alpha expressed in Escherichia coli assessed as residual activity at 10 uM (Rvb = 100 +/- 0.1%) | 2020 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2 ISSN: 1464-3405 | Synthesis and evaluation of the HIF-1α inhibitory activity of 3(5)-substituted-4-(quinolin-4-yl)- and 4-(2-phenylpyridin-4-yl)pyrazoles as inhibitors of ALK5. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425049 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425164 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1733258 | Inhibition of TGF-beta-induced morphological changes in human U-87MG cells at 0.1 to 1 uM after 48 hrs | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216ISSN: 1768-3254 | Synthesis and evaluation of the epithelial-to- mesenchymal inhibitory activity of indazole-derived imidazoles as dual ALK5/p38α MAP inhibitors. |
| 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425076 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425171 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425200 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425173 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424937 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425187 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425053 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425124 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425116 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425086 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1772982 | Inhibition of TGFBR1 (unknown origin) at 2 uM relative to control | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223ISSN: 1768-3254 | Discovery and biological evaluation of phthalazines as novel non-kinase TGFβ pathway inhibitors. |
| AID1425106 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425039 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424961 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425112 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424891 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425018 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424989 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424940 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1142668 | Antitumor activity against mouse B16 cells in mouse assessed as inhibition of tumor growth at 75 mg/kg, po bid relative to vehicle-treated control | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 ISSN: 1520-4804 | Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1563851 | Inhibition of human recombinant GST-tagged ALK5 expressed in Sf9 insect cells using casein as substrate incubated for 60 mins in presence of [33P]-ATP by radiometric assay | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180ISSN: 1768-3254 | Design, synthesis, and antifibrosis evaluation of 4-(benzo-[c][1,2,5]thiadiazol-5-yl)-3(5)-(6-methyl- pyridin-2-yl)pyrazole and 3(5)-(6-methylpyridin- 2-yl)-4-(thieno-[3,2,-c]pyridin-2-yl)pyrazole derivatives. |
| AID1425109 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424962 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425015 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1423861 | Inhibition of mouse ABL expressed in Sf9 insect cells using GGEAIYAAPFKK as substrate in presence of [gamma-33P]ATP | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127ISSN: 1768-3254 | ALK5 kinase inhibitory activity and synthesis of 2,3,4-substituted 5,5-dimethyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazoles. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1423859 | Inhibition of human ALK5 expressed in Sf9 insect cells using casein as substrate in presence of [gamma-33P]ATP | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127ISSN: 1768-3254 | ALK5 kinase inhibitory activity and synthesis of 2,3,4-substituted 5,5-dimethyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazoles. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425099 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424910 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424920 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424900 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1142655 | Selectivity index, ratio of IC50 for ALK4 (unknown origin) to IC50 for ALK5 (unknown origin) | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 ISSN: 1520-4804 | Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425029 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424970 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424930 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424890 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425212 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425035 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424947 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424997 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425093 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1733261 | Reversal of TGF-beta-induced epithelial-mesenchymal transition in human U-87MG cells assessed as reduction in vimentin protein level at 0.1 to 0.5 uM after 48 hrs by Western blotting analysis | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216ISSN: 1768-3254 | Synthesis and evaluation of the epithelial-to- mesenchymal inhibitory activity of indazole-derived imidazoles as dual ALK5/p38α MAP inhibitors. |
| AID1424895 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424985 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425197 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424950 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424953 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425096 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425155 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425133 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425064 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425023 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1142657 | Selectivity index, ratio of IC50 for RIPK2 (unknown origin) to IC50 for ALK5 (unknown origin) | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 ISSN: 1520-4804 | Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1784532 | Inhibition of human TGFbeta receptor 1 in human HEK293 cells preincubated for 24 hrs followed by addition of TGFbeta1 and measured after 24 hrs by luciferase based assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225ISSN: 1768-3254 | Discovery of 4-aminoquinolines as highly selective TGFβR1 inhibitors with an attenuated MAP4K4 profile for potential applications in immuno-oncology. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1653829 | Induction of apoptosis in human HCT116 cells assessed as early apoptotic cells at 50 uM preincubated for 12 hrs followed by TNF stimulation and measured after 24 hrs by Annexin-V/PI-staining based flow cytometric analysis (Rvb = 2.8%) | 2020 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2 ISSN: 1464-3405 | Synthesis and evaluation of the HIF-1α inhibitory activity of 3(5)-substituted-4-(quinolin-4-yl)- and 4-(2-phenylpyridin-4-yl)pyrazoles as inhibitors of ALK5. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425013 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425085 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425125 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425165 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1653825 | Induction of apoptosis in human HCT116 cells assessed as early apoptotic cells at 50 uM after 12 hrs by Annexin-V/PI-staining based flow cytometric analysis (Rvb = 1%) | 2020 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2 ISSN: 1464-3405 | Synthesis and evaluation of the HIF-1α inhibitory activity of 3(5)-substituted-4-(quinolin-4-yl)- and 4-(2-phenylpyridin-4-yl)pyrazoles as inhibitors of ALK5. |
| AID1423863 | Cytotoxicity against human MCF7 cells assessed as decrease in cell proliferation after 72 hrs by calcein AM staining-based assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127ISSN: 1768-3254 | ALK5 kinase inhibitory activity and synthesis of 2,3,4-substituted 5,5-dimethyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazoles. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424916 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1142670 | Antitumor activity against mouse B16 cells in mouse assessed as inhibition of lymph node metastasis at 75 mg/kg, po bid relative to vehicle-treated control | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 ISSN: 1520-4804 | Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425107 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425141 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1653815 | Inhibition of recombinant GST-tagged human ALK5 expressed in baculovirus infected Sf9 insect cells | 2020 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2 ISSN: 1464-3405 | Synthesis and evaluation of the HIF-1α inhibitory activity of 3(5)-substituted-4-(quinolin-4-yl)- and 4-(2-phenylpyridin-4-yl)pyrazoles as inhibitors of ALK5. |
| 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424899 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424990 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1142669 | Antitumor activity against mouse B16 cells in mouse assessed as suppression of tumor volume at 75 mg/kg, po bid relative to vehicle-treated control | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 ISSN: 1520-4804 | Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1733254 | Inhibition of recombinant human p38alpha expressed in Escherichia coli assessed as incoporation of [33]Pi after 60 mins in presence of [gamma-33P]-ATP by microplate scintillation counter method | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216ISSN: 1768-3254 | Synthesis and evaluation of the epithelial-to- mesenchymal inhibitory activity of indazole-derived imidazoles as dual ALK5/p38α MAP inhibitors. |
| AID1425008 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425003 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425138 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424922 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1784533 | Inhibition of recombinant human GST-tagged MAP4K4 expressed in baculovirus expression system using 5-FAM-KRELVEPLTPSGEAPNQALLR-CONH2 substrate preincubated for 1 hr followed by ATP and substrate addition | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225ISSN: 1768-3254 | Discovery of 4-aminoquinolines as highly selective TGFβR1 inhibitors with an attenuated MAP4K4 profile for potential applications in immuno-oncology. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425146 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425083 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424889 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424902 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1374245 | Inhibition of wild type His-tagged TGFbetaR2 (unknown origin) after 1 hr by HTRF assay | 2018 | Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5 ISSN: 1464-3391 | Heterobicyclic inhibitors of transforming growth factor beta receptor I (TGFβRI). |
| 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425055 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424897 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425017 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425130 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1256659 | Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 insect cells using casein as substrate by proprietary radioisotopic protein kinase assay | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 ISSN: 1464-3405 | Synthesis and biological evaluation of 5-(fluoro-substituted-6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)imidazoles as inhibitors of transforming growth factor-β type I receptor kinase. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425033 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1142661 | Inhibition of ALK5 in mouse 4T1 cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 ISSN: 1520-4804 | Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1653827 | Induction of apoptosis in human HCT116 cells assessed as necrotic cells at 50 uM after 12 hrs by Annexin-V/PI-staining based flow cytometric analysis (Rvb = 3.5%) | 2020 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2 ISSN: 1464-3405 | Synthesis and evaluation of the HIF-1α inhibitory activity of 3(5)-substituted-4-(quinolin-4-yl)- and 4-(2-phenylpyridin-4-yl)pyrazoles as inhibitors of ALK5. |
| AID1653813 | Inhibition of recombinant GST-tagged human ALK5 expressed in baculovirus infected Sf9 insect cells assessed as residual activity at 10 uM (Rvb = 100 +/- 0.1%) | 2020 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2 ISSN: 1464-3405 | Synthesis and evaluation of the HIF-1α inhibitory activity of 3(5)-substituted-4-(quinolin-4-yl)- and 4-(2-phenylpyridin-4-yl)pyrazoles as inhibitors of ALK5. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1634296 | Inhibition of ALK5 in human HepG2 cells assessed as reduction in TGFbeta1-induced Smad2 phosphorylation incubated for 36 hrs by Western blot analysis | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 ISSN: 1464-3405 | Synthesis and biological evaluation of novel benzo[c][1,2,5]thiadiazol-5-yl and thieno[3,2-c]- pyridin-2-yl imidazole derivatives as ALK5 inhibitors. |
| AID1534896 | Inhibition of TGFBR1 (unknown origin) | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163ISSN: 1768-3254 | Targeting the immunity protein kinases for immuno-oncology. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425071 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424918 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425014 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1634303 | Inhibition of human recombinant GST-tagged ALK5 expressed in Sf9 insect cells using casein as substrate incubated for 60 mins in presence of [33P]-ATP by scintillation counting method | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 ISSN: 1464-3405 | Synthesis and biological evaluation of novel benzo[c][1,2,5]thiadiazol-5-yl and thieno[3,2-c]- pyridin-2-yl imidazole derivatives as ALK5 inhibitors. |
| AID1563852 | Inhibition of human recombinant untagged p38alpha expressed in Escherichia coli using ATF2 as substrate incubated for 60 mins in presence of [33P]-ATP by radiometric assay | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180ISSN: 1768-3254 | Design, synthesis, and antifibrosis evaluation of 4-(benzo-[c][1,2,5]thiadiazol-5-yl)-3(5)-(6-methyl- pyridin-2-yl)pyrazole and 3(5)-(6-methylpyridin- 2-yl)-4-(thieno-[3,2,-c]pyridin-2-yl)pyrazole derivatives. |
| AID1653814 | Inhibition of recombinant human p38alpha expressed in Escherichia coli | 2020 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2 ISSN: 1464-3405 | Synthesis and evaluation of the HIF-1α inhibitory activity of 3(5)-substituted-4-(quinolin-4-yl)- and 4-(2-phenylpyridin-4-yl)pyrazoles as inhibitors of ALK5. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425072 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425160 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1142658 | Inhibition of VEGFR2 (unknown origin) by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 ISSN: 1520-4804 | Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1256662 | Inhibition of ALK5 in human HaCaT cells assessed as residual enzyme activity at 100 nM by p3TP-luciferase assay relative to control | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 ISSN: 1464-3405 | Synthesis and biological evaluation of 5-(fluoro-substituted-6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)imidazoles as inhibitors of transforming growth factor-β type I receptor kinase. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1653828 | Induction of apoptosis in human HCT116 cells assessed as viable cells at 50 uM preincubated for 12 hrs followed by TNF stimulation and measured after 24 hrs by Annexin-V/PI-staining based flow cytometric analysis (Rvb = 92.4%) | 2020 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2 ISSN: 1464-3405 | Synthesis and evaluation of the HIF-1α inhibitory activity of 3(5)-substituted-4-(quinolin-4-yl)- and 4-(2-phenylpyridin-4-yl)pyrazoles as inhibitors of ALK5. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1256660 | Inhibition of human recombinant p38alpha expressed in Escherichia coli using ATF2 as substrate by proprietary radioisotopic protein kinase assay | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 ISSN: 1464-3405 | Synthesis and biological evaluation of 5-(fluoro-substituted-6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)imidazoles as inhibitors of transforming growth factor-β type I receptor kinase. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425166 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1733255 | Inhibition of recombinant human GST-fused ALK5 expressed in baculovirus infected Sf9 cells assessed as incoporation of [33]Pi after 60 mins in presence of [gamma-33P]-ATP by microplate scintillation counter method | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216ISSN: 1768-3254 | Synthesis and evaluation of the epithelial-to- mesenchymal inhibitory activity of indazole-derived imidazoles as dual ALK5/p38α MAP 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424978 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1634306 | Inhibition of ALK5 in human SPC-A1 cells assessed as reduction in TGFbeta1-induced Smad2 phosphorylation at 0.1 to 0.5 uM incubated for 36 hrs by Western blot analysis | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 ISSN: 1464-3405 | Synthesis and biological evaluation of novel benzo[c][1,2,5]thiadiazol-5-yl and thieno[3,2-c]- pyridin-2-yl imidazole derivatives as ALK5 inhibitors. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424963 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425060 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1423860 | Inhibition of human CDK2/cyclin E expressed in Sf9 insect cells using histone H1 as substrate in presence of [gamma-33P]ATP | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127ISSN: 1768-3254 | ALK5 kinase inhibitory activity and synthesis of 2,3,4-substituted 5,5-dimethyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazoles. |
| 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1653824 | Induction of apoptosis in human HCT116 cells assessed as viable cells at 50 uM after 12 hrs by Annexin-V/PI-staining based flow cytometric analysis (Rvb = 95.3%) | 2020 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2 ISSN: 1464-3405 | Synthesis and evaluation of the HIF-1α inhibitory activity of 3(5)-substituted-4-(quinolin-4-yl)- and 4-(2-phenylpyridin-4-yl)pyrazoles as inhibitors of ALK5. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425002 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425118 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1916781 | Inhibition of human TGF-beta-R1 using TMB substrate incubated for 2.5 hrs by microplate reader analysis | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238ISSN: 1768-3254 | Recent contribution of medicinally active 2-aminothiophenes: A privileged scaffold for drug discovery. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425063 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424913 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1374244 | Inhibition of human His-tagged TGFbetaR1 T204D mutant expressed in Sf9 insect cells after 1 hr by HTRF assay | 2018 | Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5 ISSN: 1464-3391 | Heterobicyclic inhibitors of transforming growth factor beta receptor I (TGFβRI). |
| AID1256661 | Selectivity index, ratio of IC50 for human recombinant p38alpha to IC50 for human recombinant ALK5 | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 ISSN: 1464-3405 | Synthesis and biological evaluation of 5-(fluoro-substituted-6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)imidazoles as inhibitors of transforming growth factor-β type I receptor kinase. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425081 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1653830 | Induction of apoptosis in human HCT116 cells assessed as late apoptotic cells at 50 uM preincubated for 12 hrs followed by TNF stimulation and measured after 24 hrs by Annexin-V/PI-staining based flow cytometric analysis (Rvb = 1.4%) | 2020 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2 ISSN: 1464-3405 | Synthesis and evaluation of the HIF-1α inhibitory activity of 3(5)-substituted-4-(quinolin-4-yl)- and 4-(2-phenylpyridin-4-yl)pyrazoles as inhibitors of ALK5. |
| AID1563853 | Selectivity index, ratio of IC50 for human recombinant untagged p38alpha expressed in Escherichia coli to IC50 for human recombinant GST-tagged ALK5 expressed in Sf9 insect cells | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180ISSN: 1768-3254 | Design, synthesis, and antifibrosis evaluation of 4-(benzo-[c][1,2,5]thiadiazol-5-yl)-3(5)-(6-methyl- pyridin-2-yl)pyrazole and 3(5)-(6-methylpyridin- 2-yl)-4-(thieno-[3,2,-c]pyridin-2-yl)pyrazole derivatives. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425065 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424923 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425127 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425195 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424974 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425028 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425131 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1142609 | Inhibition of ALK4 (unknown origin) by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 ISSN: 1520-4804 | Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425123 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424939 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1142659 | Selectivity index, ratio of IC50 for VEGFR2 (unknown origin) to IC50 for ALK5 (unknown origin) | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 ISSN: 1520-4804 | Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425069 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424946 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425051 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1653831 | Induction of apoptosis in human HCT116 cells assessed as necrotic cells at 50 uM preincubated for 12 hrs followed by TNF stimulation and measured after 24 hrs by Annexin-V/PI-staining based flow cytometric analysis (Rvb = 3.6%) | 2020 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2 ISSN: 1464-3405 | Synthesis and evaluation of the HIF-1α inhibitory activity of 3(5)-substituted-4-(quinolin-4-yl)- and 4-(2-phenylpyridin-4-yl)pyrazoles as inhibitors of ALK5. |
| AID1424932 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1784535 | Inhibition of wild type partial length human MAP4K4 (M1 to R310 residues) expressed in bacterial expression system measured by Kinomescan assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225ISSN: 1768-3254 | Discovery of 4-aminoquinolines as highly selective TGFβR1 inhibitors with an attenuated MAP4K4 profile for potential applications in immuno-oncology. |
| AID1142656 | Inhibition of RIPK2 (unknown origin) by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 ISSN: 1520-4804 | Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425128 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425145 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425025 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425202 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425113 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1634304 | Selectivity index, ratio of IC50 for human recombinant untagged p38aplha to IC50 for human recombinant GST-tagged ALK5 | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 ISSN: 1464-3405 | Synthesis and biological evaluation of novel benzo[c][1,2,5]thiadiazol-5-yl and thieno[3,2-c]- pyridin-2-yl imidazole derivatives as ALK5 inhibitors. |
| 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425208 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| 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 ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 ISSN: 2472-5560 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 ISSN: 1521-0111 | 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 ISSN: 1091-6490 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| 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 ISSN: 1091-6490 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 ISSN: 1521-0111 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 79 (63.71) | 24.3611 |
| 2020's | 45 (36.29) | 2.80 |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 21 (16.67%) | 5.53% |
| Reviews | 7 (5.56%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 98 (77.78%) | 84.16% |
| Condition | Indicated | Studies | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Acute Disease | 0 | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Acute Edematous Pancreatitis | 0 | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Acute Myelogenous Leukemia | 0 | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Adenocarcinoma | 0 | 2019 | 2023 | 3.0 | low | 1 | 0 | 0 | 0 | 1 | 2 | |
| Adenocarcinoma, Alveolar | 0 | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
| Adenocarcinoma, Basal Cell | 0 | 2019 | 2023 | 3.0 | low | 1 | 0 | 0 | 0 | 1 | 2 | |
| Adenocarcinoma, Bronchiolo-Alveolar | 0 | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
| Androgen-Independent Prostatic Cancer | 0 | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Anemia | 0 | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Anemia, Congenital Hypoplastic, Of Blackfan And Diamond | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Anemia, Diamond-Blackfan | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Angiogenesis, Pathologic | 0 | 2016 | 2022 | 6.0 | low | 0 | 0 | 0 | 0 | 2 | 1 | |
| Arachnoidal Cerebellar Sarcoma, Circumscribed | 0 | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Astrocytoma, Grade IV | 0 | 2014 | 2022 | 5.9 | low | 2 | 0 | 0 | 0 | 5 | 3 | |
| Barrett Epithelium | 0 | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Barrett Esophagus | 0 | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Benign Cerebellar Neoplasms | 0 | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Benign Neoplasms | 0 | 2015 | 2023 | 5.9 | low | 4 | 0 | 0 | 0 | 8 | 3 | |
| Benign Neoplasms, Brain | 0 | 2015 | 2022 | 5.4 | low | 2 | 0 | 0 | 0 | 6 | 4 | |
| Bladder Cancer | 0 | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Brain Ischemia | 0 | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Brain Neoplasms | 0 | 2015 | 2022 | 5.4 | low | 2 | 0 | 0 | 0 | 6 | 4 | |
| Breast Cancer | 0 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Breast Neoplasms | 1 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Cancer of Colon | 0 | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 2 | |
| Cancer of Esophagus | 0 | 2017 | 2019 | 6.0 | low | 0 | 0 | 0 | 0 | 2 | 0 | |
| Cancer of Head | 0 | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
| Cancer of Liver | 0 | 2013 | 2021 | 5.9 | low | 5 | 0 | 0 | 0 | 14 | 3 | |
| Cancer of Lung | 0 | 2016 | 2023 | 4.8 | low | 1 | 0 | 0 | 0 | 2 | 2 | |
| Cancer of Ovary | 0 | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Cancer of Pancreas | 0 | 2016 | 2023 | 4.5 | low | 6 | 0 | 0 | 0 | 5 | 3 | |
| Cancer of Prostate | 0 | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Carcinoma, Ductal, Pancreatic | 0 | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Carcinoma, Epidermoid | 0 | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Carcinoma, Hepatocellular | 1 | 2013 | 2021 | 5.9 | low | 5 | 0 | 0 | 0 | 14 | 3 | |
| Carcinoma, Non-Small Cell Lung | 0 | 2023 | 2023 | 1.0 | low | 1 | 0 | 0 | 0 | 0 | 1 | |
| Carcinoma, Non-Small-Cell Lung | 0 | 2023 | 2023 | 1.0 | low | 1 | 0 | 0 | 0 | 0 | 1 | |
| Carcinoma, Ovarian Epithelial | 0 | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Carcinoma, Pancreatic Ductal | 0 | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Carcinoma, Squamous Cell | 0 | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Carcinoma, Squamous Cell of Head and Neck | 0 | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
| Cardiac Diseases | 0 | 2015 | 2021 | 7.0 | low | 1 | 0 | 0 | 0 | 2 | 1 | |
| Cardiovascular Stroke | 0 | 2018 | 2022 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 1 | |
| Cerebral Ischemia | 0 | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Cholangiocarcinoma | 0 | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Cholangiocellular Carcinoma | 0 | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Chronic Hepatitis | 0 | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Chronic Insomnia | 0 | 2015 | 2015 | 9.0 | low | 1 | 0 | 0 | 0 | 1 | 0 | |
| Cicatrix | 0 | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
| Cicatrization | 0 | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
| Cirrhosis | 0 | 2014 | 2022 | 4.3 | low | 0 | 0 | 0 | 0 | 3 | 3 | |
| Cirrhosis, Liver | 0 | 2017 | 2021 | 5.0 | low | 0 | 0 | 0 | 0 | 3 | 1 | |
| Colonic Inertia | 0 | 2015 | 2015 | 9.0 | low | 1 | 0 | 0 | 0 | 1 | 0 | |
| Colonic Neoplasms | 0 | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 2 | |
| Colorectal Cancer | 0 | 2016 | 2021 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 4 | |
| Colorectal Neoplasms | 0 | 2016 | 2021 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 4 | |
| Congenital Zika Syndrome | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Conjunctival Diseases | 0 | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Constipation | 0 | 2015 | 2015 | 9.0 | low | 1 | 0 | 0 | 0 | 1 | 0 | |
| Diabetes Mellitus | 0 | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Disease Exacerbation | 0 | 2019 | 2021 | 4.3 | low | 2 | 0 | 0 | 0 | 2 | 1 | |
| Disease Models, Animal | 0 | 2014 | 2022 | 6.1 | low | 0 | 0 | 0 | 0 | 7 | 1 | |
| Dysmyelopoietic Syndromes | 0 | 2011 | 2019 | 9.0 | low | 1 | 0 | 0 | 0 | 2 | 0 | |
| Ectopic Ossification | 0 | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
| Emesis | 0 | 2021 | 2021 | 3.0 | low | 1 | 0 | 0 | 0 | 0 | 1 | |
| Epiretinal Membrane | 0 | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 2 | |
| Epithelial Ovarian Cancer | 0 | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Esophageal Neoplasms | 0 | 2017 | 2019 | 6.0 | low | 0 | 0 | 0 | 0 | 2 | 0 | |
| Esophageal Squamous Cell Carcinoma | 0 | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Exanthem | 0 | 2015 | 2015 | 9.0 | low | 1 | 0 | 0 | 0 | 1 | 0 | |
| Exanthema | 0 | 2015 | 2015 | 9.0 | low | 1 | 0 | 0 | 0 | 1 | 0 | |
| Experimental Mammary Neoplasms | 0 | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Experimental Neoplasms | 0 | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Fibrosis | 0 | 2014 | 2022 | 4.3 | low | 0 | 0 | 0 | 0 | 3 | 3 | |
| Genetic Predisposition | 0 | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Germinoblastoma | 0 | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 2 | |
| Glial Cell Tumors | 0 | 2015 | 2022 | 6.5 | low | 2 | 0 | 0 | 0 | 5 | 1 | |
| Glioblastoma | 1 | 2014 | 2022 | 5.9 | low | 2 | 0 | 0 | 0 | 5 | 3 | |
| Glioma | 1 | 2015 | 2022 | 6.5 | low | 2 | 0 | 0 | 0 | 5 | 1 | |
| Head and Neck Neoplasms | 0 | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
| Heart Diseases | 0 | 2015 | 2021 | 7.0 | low | 1 | 0 | 0 | 0 | 2 | 1 | |
| Hepatitis, Chronic | 0 | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Hepatocellular Carcinoma | 0 | 2013 | 2021 | 5.9 | low | 5 | 0 | 0 | 0 | 14 | 3 | |
| Inflammation | 0 | 2019 | 2019 | 5.0 | low | 1 | 0 | 0 | 0 | 2 | 0 | |
| Injury, Ischemia-Reperfusion | 0 | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Innate Inflammatory Response | 0 | 2019 | 2019 | 5.0 | low | 1 | 0 | 0 | 0 | 2 | 0 | |
| Invasiveness, Neoplasm | 0 | 2015 | 2019 | 7.2 | low | 0 | 0 | 0 | 0 | 4 | 0 | |
| Leukemia, Myeloid, Acute | 0 | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Liver Cirrhosis | 0 | 2017 | 2021 | 5.0 | low | 0 | 0 | 0 | 0 | 3 | 1 | |
| Liver Neoplasms | 0 | 2013 | 2021 | 5.9 | low | 5 | 0 | 0 | 0 | 14 | 3 | |
| Local Neoplasm Recurrence | 0 | 2017 | 2023 | 3.7 | low | 2 | 0 | 0 | 0 | 1 | 2 | |
| Lung Neoplasms | 0 | 2016 | 2023 | 4.8 | low | 1 | 0 | 0 | 0 | 2 | 2 | |
| Lymphoma | 0 | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 2 | |
| Malignant Melanoma | 0 | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Medulloblastoma | 0 | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Melanoma | 0 | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Metastase | 0 | 2015 | 2021 | 5.2 | low | 1 | 0 | 0 | 0 | 2 | 2 | |
| Myelodysplastic Syndromes | 1 | 2011 | 2019 | 9.0 | low | 1 | 0 | 0 | 0 | 2 | 0 | |
| Myocardial Infarction | 0 | 2018 | 2022 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 1 | |
| Nausea | 0 | 2021 | 2021 | 3.0 | low | 1 | 0 | 0 | 0 | 0 | 1 | |
| Neoplasm Metastasis | 1 | 2015 | 2021 | 5.2 | low | 1 | 0 | 0 | 0 | 2 | 2 | |
| Neoplasms | 1 | 2015 | 2023 | 5.9 | low | 4 | 0 | 0 | 0 | 8 | 3 | |
| Neuroblastoma | 0 | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 2 | 0 | |
| Oral Submucous Fibrosis | 0 | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Ovarian Neoplasms | 0 | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Pancreatic Neoplasms | 1 | 2016 | 2023 | 4.5 | low | 6 | 0 | 0 | 0 | 5 | 3 | |
| Pancreatitis | 0 | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Prostatic Neoplasms | 0 | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Prostatic Neoplasms, Castration-Resistant | 1 | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Reperfusion Injury | 0 | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Response Evaluation Criteria in Solid Tumors | 0 | 2021 | 2021 | 3.0 | low | 1 | 0 | 0 | 0 | 0 | 1 | |
| Scleroderma, Systemic | 0 | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Sclerosis, Systemic | 0 | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Sensitivity and Specificity | 0 | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Sleep Initiation and Maintenance Disorders | 0 | 2015 | 2015 | 9.0 | low | 1 | 0 | 0 | 0 | 1 | 0 | |
| Squamous Cell Carcinoma of Head and Neck | 0 | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
| Urinary Bladder Neoplasms | 0 | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Vomiting | 0 | 2021 | 2021 | 3.0 | low | 1 | 0 | 0 | 0 | 0 | 1 | |
| Zika Virus Infection | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Article | Year |
|---|---|
| Efficacy and safety of abemaciclib alone and with PI3K/mTOR inhibitor LY3023414 or galunisertib versus chemotherapy in previously treated metastatic pancreatic adenocarcinoma: A randomized controlled trial. Cancer medicine, , Volume: 12, Issue:20 | 2023 |
| Safety and activity of the TGFβ receptor I kinase inhibitor galunisertib plus the anti-PD-L1 antibody durvalumab in metastatic pancreatic cancer. Journal for immunotherapy of cancer, , Volume: 9, Issue:3 | 2021 |
| Cardiac Safety of TGF-β Receptor I Kinase Inhibitor LY2157299 Monohydrate in Cancer Patients in a First-in-Human Dose Study. Cardiovascular toxicology, , Volume: 15, Issue:4 | 2015 |
| Article | Year |
|---|---|
| Population pharmacokinetics and exposure-overall survival analysis of the transforming growth factor-β inhibitor galunisertib in patients with pancreatic cancer. Cancer chemotherapy and pharmacology, , Volume: 84, Issue:5 | 2019 |
| Pharmacokinetic, pharmacodynamic and biomarker evaluation of transforming growth factor-β receptor I kinase inhibitor, galunisertib, in phase 1 study in patients with advanced cancer. Investigational new drugs, , Volume: 33, Issue:2 | 2015 |
| Defining a therapeutic window for the novel TGF-β inhibitor LY2157299 monohydrate based on a pharmacokinetic/pharmacodynamic model. British journal of clinical pharmacology, , Volume: 77, Issue:5 | 2014 |
| Effect of gastric pH on the pharmacokinetics of a BCS class II compound in dogs: utilization of an artificial stomach and duodenum dissolution model and GastroPlus,™ simulations to predict absorption. Journal of pharmaceutical sciences, , Volume: 100, Issue:11 | 2011 |
| Article | Year |
|---|---|
| A phase Ib/II study of galunisertib in combination with nivolumab in solid tumors and non-small cell lung cancer. BMC cancer, , Jul-28, Volume: 23, Issue:1 | 2023 |
| Phase 1b/2a study of galunisertib, a small molecule inhibitor of transforming growth factor-beta receptor I, in combination with standard temozolomide-based radiochemotherapy in patients with newly diagnosed malignant glioma. Investigational new drugs, , Volume: 38, Issue:5 | 2020 |
| A phase 1b study of transforming growth factor-beta receptor I inhibitor galunisertib in combination with sorafenib in Japanese patients with unresectable hepatocellular carcinoma. Investigational new drugs, , Volume: 37, Issue:1 | 2019 |
| Phase 1b study of galunisertib in combination with gemcitabine in Japanese patients with metastatic or locally advanced pancreatic cancer. Cancer chemotherapy and pharmacology, , Volume: 79, Issue:6 | 2017 |