PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 26703450-3 2016 Pufferfish that received rIFN-gamma injection had an elevated phagocytic activity at 1 and 3 dpi, whereas rIFN-gammarel and rIL-4/13A treated fish showed an increased phagocytic activity only at 1 and 3 dpi, respectively. 13a 130-133 interleukin 4 Rattus norvegicus 124-129 27782099-4 2016 Further structure-based optimization revealed that 6-(2,6-dichloro-3,5-dimethoxyphenyl)-N-(3-(4-methylpiperazin-1-yl)phenyl)-1H-indazole-4-carboxamide (13a) is the most potent FGFR1 inhibitor in this series, with an enzyme inhibitory activity IC50 value of about 30.2 nM. 13a 152-155 fibroblast growth factor receptor 1 Homo sapiens 176-181 26703450-4 2016 Superoxide anion production increased only at 1 dpi in rIFN-gamma, rIFN-gammarel and rIL-4/13A injected pufferfish. 13a 91-94 interleukin 4 Rattus norvegicus 85-90 20536349-5 2010 Reporter assays demonstrated that compound 13a successfully relieved transcriptional repression by RAR-alpha, while 13b and 13c could not, demonstrating the critical role of the acid moiety in this binding. 13a 43-46 retinoic acid receptor alpha Homo sapiens 99-108 23856049-3 2013 These efforts culminated in the discovery of compound 13a, a potent, relatively selective inhibitor of TAK1 with good pharmacokinetic properties in mice, which was active in an in vivo model of ovarian cancer. 13a 54-57 mitogen-activated protein kinase kinase kinase 7 Mus musculus 103-107 25419444-3 2014 We believe 13a represents a useful probe for interrogating STAT5 function in cells as well as being a potential candidate for advanced preclinical trials. 13a 11-14 signal transducer and activator of transcription 5A Homo sapiens 59-64 19343204-10 2009 As proteins, either ME-13a- or ME-13b-containing isoform can cell-autonomously rescue the embryonic lethality caused by genetic loss of N-Cadherin. 13a 23-26 Cadherin-N Drosophila melanogaster 136-146 20097709-12 2010 Insulin (5-10 nm) suppressed all TCF7L2 isoforms in SGBS cells but suppressed exon 13a-containing isoforms most significantly (P < 0.001). 13a 83-86 insulin Homo sapiens 0-7 17409557-2 2007 Among the various fused furan derivatives synthesized, a benzothieno[3,2-b]furan derivative 13a displayed potent inhibitory activity towards IKKbeta in enzymatic and cellular assays. 13a 92-95 inhibitor of nuclear factor kappa B kinase subunit beta Homo sapiens 141-148 33272706-4 2021 Analogues with cyclohexylaminoethoxy (13a) or adamantylaminoethoxy BSC (13b) lacking a polar aromatic ring displayed high ER-binding affinity and ER antagonism in Ishikawa cells higher than raloxifene and similar to fulvestrant (ICI182,780). 13a 38-41 epiregulin Homo sapiens 122-124 17173447-6 2006 The pKa* of the coordinated water in [(eta6-p-cym)Ru(azpyz-NMe2)OH2]2+ (13A) is 4.60, consistent with the increased acidity of the ruthenium center upon coordination to the azo ligand. 13a 72-75 NME/NM23 nucleoside diphosphate kinase 2 Homo sapiens 59-63 34378541-5 2021 In comparison with the well-known BRD4 inhibitor (+)-JQ1, 13a showed more potent anticancer activity in NF-kappaB-active MDA-MB-231 cells. 13a 58-61 nuclear factor kappa B subunit 1 Homo sapiens 104-113 9658576-9 1998 These data suggest that 13a may be an useful agent for the treatment of angiotensin II-dependent diseases, such as hypertension. 13a 24-27 angiotensinogen Rattus norvegicus 72-86 34628225-5 2021 Molecular docking analysis suggested that 13a could interact with the catalytic active sites and the peripheral anion site of AChE, and bind to Abeta1-42 pentamers. 13a 42-45 acetylcholinesterase Mus musculus 126-130 34628225-6 2021 Moreover, 13a effectively attenuated Abeta1-42 oligomers-induced cognitive dysfunction in mice by activating the cAMP-response element binding protein/brain-derived neurotrophic factor signaling pathway, decreasing tau phosphorylation, preventing synaptic toxicity, and inhibiting neuroinflammation. 13a 10-13 brain derived neurotrophic factor Mus musculus 151-184 35489222-4 2022 Through structure-activity relationship studies, the most optimized compound 13a was developed as a potent inhibitor at FLT3 and FLT3/D835Y with IC50 values of 0.26 nM and 0.18 nM, respectively, which also displayed remarkably strong in vitro anticancer activities, with single-digit nanomolar GI50 values for several AML (MV4-11 and MOLM14) and Ba/F3 cell lines expressed with secondary TKD mutated FLT3 kinases as well as FLT3-ITD. 13a 77-80 fms related receptor tyrosine kinase 3 Homo sapiens 120-124 35489222-4 2022 Through structure-activity relationship studies, the most optimized compound 13a was developed as a potent inhibitor at FLT3 and FLT3/D835Y with IC50 values of 0.26 nM and 0.18 nM, respectively, which also displayed remarkably strong in vitro anticancer activities, with single-digit nanomolar GI50 values for several AML (MV4-11 and MOLM14) and Ba/F3 cell lines expressed with secondary TKD mutated FLT3 kinases as well as FLT3-ITD. 13a 77-80 fms related receptor tyrosine kinase 3 Homo sapiens 129-133 35489222-4 2022 Through structure-activity relationship studies, the most optimized compound 13a was developed as a potent inhibitor at FLT3 and FLT3/D835Y with IC50 values of 0.26 nM and 0.18 nM, respectively, which also displayed remarkably strong in vitro anticancer activities, with single-digit nanomolar GI50 values for several AML (MV4-11 and MOLM14) and Ba/F3 cell lines expressed with secondary TKD mutated FLT3 kinases as well as FLT3-ITD. 13a 77-80 FMS-like tyrosine kinase 3 Mus musculus 400-404 35489222-4 2022 Through structure-activity relationship studies, the most optimized compound 13a was developed as a potent inhibitor at FLT3 and FLT3/D835Y with IC50 values of 0.26 nM and 0.18 nM, respectively, which also displayed remarkably strong in vitro anticancer activities, with single-digit nanomolar GI50 values for several AML (MV4-11 and MOLM14) and Ba/F3 cell lines expressed with secondary TKD mutated FLT3 kinases as well as FLT3-ITD. 13a 77-80 FMS-like tyrosine kinase 3 Mus musculus 424-428 35489222-6 2022 Furthermore, significant in vivo anticancer efficacy of compound 13a was confirmed in a xenograft animal model implanted with FLT3-ITD/D835Y-expressing MOLM-14 cells related to secondary TKD mutation. 13a 65-68 fms related receptor tyrosine kinase 3 Homo sapiens 126-130 33272706-4 2021 Analogues with cyclohexylaminoethoxy (13a) or adamantylaminoethoxy BSC (13b) lacking a polar aromatic ring displayed high ER-binding affinity and ER antagonism in Ishikawa cells higher than raloxifene and similar to fulvestrant (ICI182,780). 13a 38-41 epiregulin Homo sapiens 146-148 32631508-4 2020 Further exploration of possible mechanism of action indicates that 13a not only activates ROS production through NQO1-directed redox cycling but also inhibits the phosphorylation of STAT3. 13a 67-70 NAD(P)H quinone dehydrogenase 1 Homo sapiens 113-117 32886510-7 2020 Liquid chromatography-mass spectrometry (LC-MS) analysis confirmed that 13a modified selenocysteine 498 (U) residues in the redox centers of TrxR, resulting in enzyme inhibition. 13a 72-75 peroxiredoxin 5 Homo sapiens 141-145 32886510-8 2020 Therefore, compound 13a acts as a novel TrxR inhibitor and may be a promising candidate for cancer intervention. 13a 20-23 peroxiredoxin 5 Homo sapiens 40-44 32912435-7 2020 All the results showed that 13a was a promising EGFR inhibitor. 13a 28-31 epidermal growth factor receptor Homo sapiens 48-52 32631508-5 2020 These findings indicate that 13a has potential use for the development of new skeleton drug candidate as an efficient substrate of NQO1 and STAT3 inhibitor. 13a 29-32 NAD(P)H quinone dehydrogenase 1 Homo sapiens 131-135 32631508-4 2020 Further exploration of possible mechanism of action indicates that 13a not only activates ROS production through NQO1-directed redox cycling but also inhibits the phosphorylation of STAT3. 13a 67-70 signal transducer and activator of transcription 3 Homo sapiens 182-187 32631508-5 2020 These findings indicate that 13a has potential use for the development of new skeleton drug candidate as an efficient substrate of NQO1 and STAT3 inhibitor. 13a 29-32 signal transducer and activator of transcription 3 Homo sapiens 140-145 30360747-18 2019 Among these compounds the derivative 13a showed best IC50 value of 63.34 microg mL-1 (182.86 microM). 13a 37-40 L1 cell adhesion molecule Mus musculus 80-84 32321249-3 2020 Lead inhibitor 13a shows picomolar or low nanomolar IC50 against HDAC1 and HDAC3 and exhibits differential toxicity profiles toward multiple cancer cells with different FLT3 and p53 status. 13a 15-18 histone deacetylase 1 Homo sapiens 65-70 32321249-3 2020 Lead inhibitor 13a shows picomolar or low nanomolar IC50 against HDAC1 and HDAC3 and exhibits differential toxicity profiles toward multiple cancer cells with different FLT3 and p53 status. 13a 15-18 histone deacetylase 3 Homo sapiens 75-80 30885648-7 2019 Furthermore, the docking results of 13a revealed that the oxygen atom at the position of C-3 connected to the heme of CYP17, which may be helpful for its satisfactory dual-target inhibition. 13a 36-39 cytochrome P450 family 17 subfamily A member 1 Homo sapiens 118-123 32321249-3 2020 Lead inhibitor 13a shows picomolar or low nanomolar IC50 against HDAC1 and HDAC3 and exhibits differential toxicity profiles toward multiple cancer cells with different FLT3 and p53 status. 13a 15-18 fms related receptor tyrosine kinase 3 Homo sapiens 169-173 32321249-3 2020 Lead inhibitor 13a shows picomolar or low nanomolar IC50 against HDAC1 and HDAC3 and exhibits differential toxicity profiles toward multiple cancer cells with different FLT3 and p53 status. 13a 15-18 tumor protein p53 Homo sapiens 178-181 32321249-4 2020 13a indirectly inhibits the FLT3 signaling pathway and down-regulates the master anti-apoptotic proteins, resulting in the activation of pro-caspase3 in in wt-p53 FLT3-ITD MV4-11 cells. 13a 0-3 fms related receptor tyrosine kinase 3 Homo sapiens 28-32 32321249-4 2020 13a indirectly inhibits the FLT3 signaling pathway and down-regulates the master anti-apoptotic proteins, resulting in the activation of pro-caspase3 in in wt-p53 FLT3-ITD MV4-11 cells. 13a 0-3 caspase 3 Homo sapiens 141-149 32321249-4 2020 13a indirectly inhibits the FLT3 signaling pathway and down-regulates the master anti-apoptotic proteins, resulting in the activation of pro-caspase3 in in wt-p53 FLT3-ITD MV4-11 cells. 13a 0-3 tumor protein p53 Homo sapiens 159-162 32321249-4 2020 13a indirectly inhibits the FLT3 signaling pathway and down-regulates the master anti-apoptotic proteins, resulting in the activation of pro-caspase3 in in wt-p53 FLT3-ITD MV4-11 cells. 13a 0-3 fms related receptor tyrosine kinase 3 Homo sapiens 163-167 32321249-6 2020 The MDM2 antagonist and the proteasome inhibitor promote 13a-triggered apoptosis by preventing p53 degradation. 13a 57-60 MDM2 proto-oncogene Homo sapiens 4-8 32321249-6 2020 The MDM2 antagonist and the proteasome inhibitor promote 13a-triggered apoptosis by preventing p53 degradation. 13a 57-60 tumor protein p53 Homo sapiens 95-98 29983575-0 2018 CAT3, a prodrug of 13a(S)-3-hydroxyl-6,7-dimethoxyphenanthro[9,10-b]-indolizidine, circumvents temozolomide-resistant glioblastoma via the Hedgehog signaling pathway, independently of O6-methylguanine DNA methyltransferase expression. 13a 19-22 solute carrier family 7 member 3 Homo sapiens 0-4 29983575-0 2018 CAT3, a prodrug of 13a(S)-3-hydroxyl-6,7-dimethoxyphenanthro[9,10-b]-indolizidine, circumvents temozolomide-resistant glioblastoma via the Hedgehog signaling pathway, independently of O6-methylguanine DNA methyltransferase expression. 13a 19-22 O-6-methylguanine-DNA methyltransferase Homo sapiens 184-222 29235893-4 2018 RESULTS & DISCUSSION: The furoaurone derivative, 13a was the most active one exhibiting promising growth inhibition against leukemia, K562 and melanoma, MDA-MB-435 cells at concentration of 10 muM. 13a 53-56 latexin Homo sapiens 197-200 29235893-7 2018 Simulation docking study was undertaken to gain insight into the possible binding mode of 13a in the CDK2 enzyme. 13a 90-93 cyclin dependent kinase 2 Homo sapiens 101-105 29944015-6 2018 Also, 13a displayed significant increase in the percentage of annexin V-FITC positive apoptotic cells from 1.75-13.76%. 13a 6-9 annexin A5 Homo sapiens 62-71