Assay ID | Title | Year | Journal | Article |
AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
| Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347111 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347126 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347117 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347123 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
AID1347110 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347124 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347118 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347127 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347115 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347128 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347109 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347119 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4
| A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347114 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347121 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347116 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347129 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347113 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347112 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347125 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347122 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1542201 | Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability after 96 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Discovery of deshydroxy bicalutamide derivatives as androgen receptor antagonists. |
AID1635251 | Antiproliferative activity against human DU145 cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID1187565 | Inhibition of androgen receptor in human LNCAP cells assessed as reduction in PSA mRNA level at 10 to 20 uM after 24 hrs by RT-PCR analysis | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
| A new avenue toward androgen receptor pan-antagonists: C2 sterically hindered substitution of hydroxy-propanamides. |
AID1635239 | Antagonist activity at rat androgen receptor fused with DNA-binding domain of GAL4 expressed in AR-UAS-bla GripTite 293 cells assessed as inhibition of R1881-induced receptor activation at 10 uM preincubated for 30 mins followed by R1881 addition measured | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID1635253 | Antiproliferative activity against human VCaP cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID1635223 | Antiproliferative activity against human VCaP cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID1635221 | Antiproliferative activity against human DU145 cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID1569750 | Metabolic stability in liver microsomes (unknown origin) assessed as intrinsic clearance per mg of protein at 3 uM measured upto 45 mins in presence of NADPH by LC-MS/MS analysis | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | A new series of bicalutamide, enzalutamide and enobosarm derivatives carrying pentafluorosulfanyl (SF |
AID1313192 | Inhibition of human ERG transfected in CHO cells assessed as blockade of tail current at 25 uM by patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
| Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety. |
AID1187551 | Inhibition of R1881-induced migration of human LNCAP cells at 10 uM by transwell assay | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
| A new avenue toward androgen receptor pan-antagonists: C2 sterically hindered substitution of hydroxy-propanamides. |
AID1569744 | Antiproliferative activity against human DU145 cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | A new series of bicalutamide, enzalutamide and enobosarm derivatives carrying pentafluorosulfanyl (SF |
AID1635250 | Antiproliferative activity against human LNCAP cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID711907 | Inhibition of androgen receptor in human LNCaP-AR cells assessed as reduction in prostate specific antigen secretion at 20 uM after 48 hrs by spectrophotometric analysis | 2012 | ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6
| Nonsteroidal androgen receptor ligands: versatile syntheses and biological data. |
AID1313184 | Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay | 2016 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
| Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety. |
AID1635260 | Antagonist activity at rat androgen receptor fused with DNA-binding domain of GAL4 expressed in AR-UAS-bla GripTite 293 cells assessed as inhibition of R1881-induced receptor activation at 10 nM preincubated for 30 mins followed by R1881 addition measured | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID1635248 | Efflux ratio of apparent permeability from basolateral to apical side over apical to basolateral side in human Caco2 cells at 10 uM incubated for 120 mins by LC-MS/MS analysis | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID293945 | Binding affinity to human AR | 2007 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
| Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones. |
AID1362956 | Antagonist activity at AR T877A mutant in human LNCAP cells assessed as inhibition of DHT-induced cell proliferation treated for 3 days followed by compound washout and supplemented with fresh medium containing compound measured after 3 days by WST8 assay | 2018 | Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18
| Structure-activity relationship of novel (benzoylaminophenoxy)phenol derivatives as anti-prostate cancer agents. |
AID1569745 | Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | A new series of bicalutamide, enzalutamide and enobosarm derivatives carrying pentafluorosulfanyl (SF |
AID1430114 | Selectivity index, ratio of IC50 for mouse 3T3 cells to IC50 for AR T877A mutant in human LNCAP cells | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
| Design, synthesis and biological evaluation of 2-(4-phenylthiazol-2-yl) isoindoline-1,3-dione derivatives as anti-prostate cancer agents. |
AID1635263 | Antagonist activity at rat androgen receptor fused with DNA-binding domain of GAL4 expressed in AR-UAS-bla GripTite 293 cells assessed as inhibition of R1881-induced receptor activation at 0.316 nM preincubated for 30 mins followed by R1881 addition measu | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID298547 | Antagonist activity at human androgen receptor by luciferase reporter gene assay | 2007 | Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
| Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators. |
AID1187567 | Antitumor activity against human VCaP cells xenografted in CD-1 nu/nu mouse assessed as tumor regression at 10 mg/kg, po for 4 consecutive weeks starting on day 35 of tumor implantation measured after 100 days | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
| A new avenue toward androgen receptor pan-antagonists: C2 sterically hindered substitution of hydroxy-propanamides. |
AID1313187 | Antagonist activity at GAL4 DBD-fused androgen receptor LBD (unknown origin) transfected in UAS-bla GripTite 293 cells assessed as inhibition of R1881-induced receptor activation after 16 to 24 hrs by beta-lactamase reporter gene assay | 2016 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
| Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety. |
AID1635254 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability at 100 uM after 72 hrs by MTT assay relative to control | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID1250205 | Antagonist activity at AR T877A mutant expressed in human LNCaP cells assessed as inhibition of 10 nM DHT-stimulated cell proliferation after 6 days by WST-8 assay | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Design and synthesis of 4-benzyl-1-(2H)-phthalazinone derivatives as novel androgen receptor antagonists. |
AID1187556 | Growth inhibition of human LNCaP-AR cells expressing wild-type androgen receptor after 144 hrs by SRB assay | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
| A new avenue toward androgen receptor pan-antagonists: C2 sterically hindered substitution of hydroxy-propanamides. |
AID711913 | Induction of apoptosis in human LNCAP cells at 20 uM after 144 hrs by propidium iodide staining based flow cytometry analysis | 2012 | ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6
| Nonsteroidal androgen receptor ligands: versatile syntheses and biological data. |
AID1542202 | Antiproliferative activity against human PC3 cells assessed as reduction in cell viability after 96 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Discovery of deshydroxy bicalutamide derivatives as androgen receptor antagonists. |
AID1635255 | Antagonist activity at rat androgen receptor fused with DNA-binding domain of GAL4 expressed in AR-UAS-bla GripTite 293 cells assessed as inhibition of R1881-induced receptor activation at 3160 nM preincubated for 30 mins followed by R1881 addition measur | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID1635220 | Antiproliferative activity against human 22Rv1 cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID1187562 | Inhibition of cell survival in human VCaP cells after 144 hrs by TUNEL assay | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
| A new avenue toward androgen receptor pan-antagonists: C2 sterically hindered substitution of hydroxy-propanamides. |
AID1635259 | Antagonist activity at rat androgen receptor fused with DNA-binding domain of GAL4 expressed in AR-UAS-bla GripTite 293 cells assessed as inhibition of R1881-induced receptor activation at 31.6 nM preincubated for 30 mins followed by R1881 addition measur | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID293944 | Antagonist activity at human AR assessed as inhibition of DHT-induced response | 2007 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
| Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones. |
AID1313193 | Protein binding in human plasma by equilibrium dialysis method | 2016 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
| Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety. |
AID1569747 | Antiproliferative activity against human VCaP cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | A new series of bicalutamide, enzalutamide and enobosarm derivatives carrying pentafluorosulfanyl (SF |
AID1635222 | Antiproliferative activity against human LNCAP cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID711914 | Induction of apoptosis in human LNCaP-AR cells at 20 uM after 144 hrs by propidium iodide staining based flow cytometry analysis | 2012 | ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6
| Nonsteroidal androgen receptor ligands: versatile syntheses and biological data. |
AID293941 | Agonist activity at human AR | 2007 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
| Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones. |
AID711910 | Cytocidal activity in against human LNCAP cells after 144 hrs by SRB assay | 2012 | ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6
| Nonsteroidal androgen receptor ligands: versatile syntheses and biological data. |
AID1635257 | Antagonist activity at rat androgen receptor fused with DNA-binding domain of GAL4 expressed in AR-UAS-bla GripTite 293 cells assessed as inhibition of R1881-induced receptor activation at 316 nM preincubated for 30 mins followed by R1881 addition measure | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID1885040 | Binding affinity to Androgen receptor (unknown origin) | 2022 | Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
| Therapeutic Strategies to Target the Androgen Receptor. |
AID1569821 | Protein binding in human plasma | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | A new series of bicalutamide, enzalutamide and enobosarm derivatives carrying pentafluorosulfanyl (SF |
AID1569753 | Inhibition of human ERG expressed in CHO cells at 25 uM by whole-cell voltage-clamp analysis relative to control | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | A new series of bicalutamide, enzalutamide and enobosarm derivatives carrying pentafluorosulfanyl (SF |
AID711909 | Cytotoxicity against human LNCaP-AR cells assessed as growth inhibition at 2 to 20 uM after 144 hrs by SRB assay relative to control | 2012 | ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6
| Nonsteroidal androgen receptor ligands: versatile syntheses and biological data. |
AID694143 | Displacement of [3H]R1881 from wild type human androgen receptor expressed in COS-1 cells co-transfected with pSG5 after 15 mins by scintillation assay | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| Design, synthesis, and biological evaluation of nonsteroidal cycloalkane[d]isoxazole-containing androgen receptor modulators. |
AID1888465 | Anti-androgenic activity at androgen receptor (unknown origin) expressed in HEK293 cells by BRET assay | 2022 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 55 | Dual-function antiandrogen/HDACi hybrids based on enzalutamide and entinostat. |
AID1635249 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID1416294 | Antiproliferative activity against human VCaP cells after 96 hrs by propidium iodide staining-based fluorescence assay | 2017 | MedChemComm, Jul-01, Volume: 8, Issue:7
| Rational design and synthesis of novel phenylsulfonyl-benzamides as anti-prostate cancer agents. |
AID1313183 | Antiproliferative activity against human DU145 cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay | 2016 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
| Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety. |
AID1635258 | Antagonist activity at rat androgen receptor fused with DNA-binding domain of GAL4 expressed in AR-UAS-bla GripTite 293 cells assessed as inhibition of R1881-induced receptor activation at 100 nM preincubated for 30 mins followed by R1881 addition measure | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID293943 | Antagonist activity at human AR | 2007 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
| Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones. |
AID1313182 | Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay | 2016 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
| Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety. |
AID1442880 | Antagonist activity at androgen receptor V7 mutant in human CW22Rv1 cells assessed as cell growth inhibition after 72 hrs by SRB assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| 1,4-Substituted Triazoles as Nonsteroidal Anti-Androgens for Prostate Cancer Treatment. |
AID1313186 | Antagonist activity at GAL4 DBD-fused androgen receptor LBD (unknown origin) transfected in UAS-bla GripTite 293 cells assessed as inhibition of R1881-induced receptor activation at 10 uM after 16 to 24 hrs by beta-lactamase reporter gene assay | 2016 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
| Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety. |
AID1635252 | Antiproliferative activity against human 22Rv1 cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID1187531 | Antagonist activity at wild-type human androgen receptor expressed in COS7 cells assessed as inhibition of R1881-induced gene expression at 10 nM to 10 uM after 24 hrs by luciferase reporter assay | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
| A new avenue toward androgen receptor pan-antagonists: C2 sterically hindered substitution of hydroxy-propanamides. |
AID298545 | Agonist activity at human androgen receptor by luciferase reporter gene assay | 2007 | Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
| Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators. |
AID318061 | Antiproliferative activity against human PC3 cells at 10 uM after 5 days | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Synthesis and structure-activity relationships of the first ferrocenyl-aryl-hydantoin derivatives of the nonsteroidal antiandrogen nilutamide. |
AID293942 | Agonist activity at human AR relative to DHT | 2007 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
| Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones. |
AID1430124 | Antagonist activity at AR T877A mutant in human LNCAP cells assessed as inhibition of DHT-induced Cyclin D1 mRNA level at 5 uM after 24 hrs by SYBR Green dye based qPCR method | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
| Design, synthesis and biological evaluation of 2-(4-phenylthiazol-2-yl) isoindoline-1,3-dione derivatives as anti-prostate cancer agents. |
AID305972 | Inhibition of prostate weight in immature Sprague-Dawley rat at 2 mg/day, sc relative to testosterone | 2007 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
| Synthesis of potent and tissue-selective androgen receptor modulators (SARMs): 2-(2,2,2)-Trifluoroethyl-benzimidazole scaffold. |
AID1635243 | Intrinsic clearance in human liver microsomes assessed per mg protein at 3 uM preincubated with compound followed by NADPH addition measured after 5 to 45 mins by LC-MS/MS analysis | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID1187558 | Growth inhibition of human VCaP cells after 144 hrs by SRB assay | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
| A new avenue toward androgen receptor pan-antagonists: C2 sterically hindered substitution of hydroxy-propanamides. |
AID1187543 | Cytotoxicity against human DU145 cells after 144 hrs by SRB assay | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
| A new avenue toward androgen receptor pan-antagonists: C2 sterically hindered substitution of hydroxy-propanamides. |
AID1430111 | Antagonist activity at AR T877A mutant in human LNCAP cells assessed as inhibition of DHT-induced proliferation after 48 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
| Design, synthesis and biological evaluation of 2-(4-phenylthiazol-2-yl) isoindoline-1,3-dione derivatives as anti-prostate cancer agents. |
AID1187557 | Growth inhibition of (R)-bicalutamide-resisitant human LNCAP cells after 144 hrs by SRB assay | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
| A new avenue toward androgen receptor pan-antagonists: C2 sterically hindered substitution of hydroxy-propanamides. |
AID296865 | Inhibition of prostate weight in intact Sprague-Dawley rat at 30 mg/kg relative to control | 2007 | Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16
| Design, synthesis, and in vivo SAR of a novel series of pyrazolines as potent selective androgen receptor modulators. |
AID375616 | Half life in human | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit. |
AID1569751 | Metabolic stability in liver microsomes (unknown origin) assessed as half life at 3 uM measured upto 45 mins in presence of NADPH by LC-MS/MS analysis | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | A new series of bicalutamide, enzalutamide and enobosarm derivatives carrying pentafluorosulfanyl (SF |
AID1187561 | Inhibition of cell survival in (R)-bicalutamide-resisitant human LNCAP cells after 144 hrs by TUNEL assay | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
| A new avenue toward androgen receptor pan-antagonists: C2 sterically hindered substitution of hydroxy-propanamides. |
AID1187555 | Growth inhibition of human LNCAP cells expressing mutant androgen receptor after 144 hrs by SRB assay | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
| A new avenue toward androgen receptor pan-antagonists: C2 sterically hindered substitution of hydroxy-propanamides. |
AID292766 | Inhibition of testosterone-enhanced ventral prostate weight in castrated immature Sprague-Dawley rat | 2007 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
| Serendipitous discovery of novel imidazolopyrazole scaffold as selective androgen receptor modulators. |
AID318060 | Displacement of [3H]DHT from androgen receptor | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Synthesis and structure-activity relationships of the first ferrocenyl-aryl-hydantoin derivatives of the nonsteroidal antiandrogen nilutamide. |
AID339521 | Antagonist activity at wild type human recombinant androgen receptor assessed as inhibition of testosterone-induced growth of mouse androgen dependent SC3 cells by WST-1 method | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14
| 4-(Anilino)pyrrole-2-carboxamides: Novel non-steroidal/non-anilide type androgen antagonists effective upon human prostate tumor LNCaP cells with mutated nuclear androgen receptor. |
AID711906 | Inhibition of androgen receptor in human LNCAP cells assessed as reduction in prostate specific antigen secretion at 20 uM after 48 hrs by spectrophotometric analysis | 2012 | ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6
| Nonsteroidal androgen receptor ligands: versatile syntheses and biological data. |
AID318063 | Partition coefficient, log P of the compound | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Synthesis and structure-activity relationships of the first ferrocenyl-aryl-hydantoin derivatives of the nonsteroidal antiandrogen nilutamide. |
AID1635247 | Apparent permeability from basolateral to apical side in human Caco2 cells at 10 uM incubated for 120 mins by LC-MS/MS analysis | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID39292 | Binding Affinity towards Rat Androgen Receptor was determined using [3H]- mibolerone as radioligand. | 2000 | Journal of medicinal chemistry, Feb-24, Volume: 43, Issue:4
| Chiral nonsteroidal affinity ligands for the androgen receptor. 1. Bicalutamide analogues bearing electrophilic groups in the B aromatic ring. |
AID1635264 | Apparent permeability from apical to basolateral side in human Caco2 cells at 100 uM incubated for 120 mins by UV spectroscopic analysis | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID1416291 | Antiproliferative activity against human 22Rv1 cells after 96 hrs by propidium iodide staining-based fluorescence assay | 2017 | MedChemComm, Jul-01, Volume: 8, Issue:7
| Rational design and synthesis of novel phenylsulfonyl-benzamides as anti-prostate cancer agents. |
AID1635241 | Antagonist activity at rat androgen receptor fused with DNA-binding domain of GAL4 expressed in AR-UAS-bla GripTite 293 cells assessed as inhibition of R1881-induced receptor activation preincubated for 30 mins followed by R1881 addition measured after 16 | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID1542200 | Antiproliferative activity against human VCaP cells assessed as reduction in cell viability after 96 hrs by MTS assay | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Discovery of deshydroxy bicalutamide derivatives as androgen receptor antagonists. |
AID1313190 | Cytotoxicity against human HepG2 cells assessed as cell viability after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
| Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety. |
AID305973 | Stimulation of levator ani muscle weight in immature Sprague-Dawley rat at 2 mg/day relative to testosterone | 2007 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
| Synthesis of potent and tissue-selective androgen receptor modulators (SARMs): 2-(2,2,2)-Trifluoroethyl-benzimidazole scaffold. |
AID1187566 | Inhibition of androgen receptor in (R)-bicalutamide-resisitant human LNCAP cells assessed as reduction in PSA mRNA level at 10 to 20 uM after 24 hrs by RT-PCR analysis | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
| A new avenue toward androgen receptor pan-antagonists: C2 sterically hindered substitution of hydroxy-propanamides. |
AID1313185 | Antiproliferative activity against human VCaP cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay | 2016 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
| Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety. |
AID1187544 | Cytotoxicity against human PC3 cells after 144 hrs by SRB assay | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
| A new avenue toward androgen receptor pan-antagonists: C2 sterically hindered substitution of hydroxy-propanamides. |
AID1569746 | Antiproliferative activity against human LNCAP cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | A new series of bicalutamide, enzalutamide and enobosarm derivatives carrying pentafluorosulfanyl (SF |
AID298546 | Agonist efficacy at human androgen receptor by luciferase reporter gene assay relative to DHT | 2007 | Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
| Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators. |
AID694142 | Displacement of [3H]R1881 from wild type human androgen receptor expressed in COS-1 cells co-transfected with pSG5 after 15 mins by scintillation assay relative to untreated control | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| Design, synthesis, and biological evaluation of nonsteroidal cycloalkane[d]isoxazole-containing androgen receptor modulators. |
AID1635265 | Efflux ratio of apparent permeability from basolateral to apical side over apical to basolateral side in human Caco2 cells at 100 uM incubated for 120 mins by UV spectroscopic analysis | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID491347 | Displacement of [3H]dihydrotestosterone from GST-tagged human androgen receptor expressed in Escherichia coli HB101 at 10 uM by liquid scintillation counting relative to dihydrotestosterone | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13
| Design and synthesis of androgen receptor full antagonists bearing a p-carborane cage: promising ligands for anti-androgen withdrawal syndrome. |
AID1430112 | Antiproliferative activity against AR negative human PC3 cells after 48 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
| Design, synthesis and biological evaluation of 2-(4-phenylthiazol-2-yl) isoindoline-1,3-dione derivatives as anti-prostate cancer agents. |
AID176507 | Antiandrogen activity in male rats | 1988 | Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
| Resolution of the nonsteroidal antiandrogen 4'-cyano-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methyl-3'- (trifluoromethyl)-propionanilide and the determination of the absolute configuration of the active enantiomer. |
AID1187532 | Antagonist activity at wild-type androgen receptor (unknown origin) expressed in human LNCaP cells assessed as inhibition of R1881-induced gene expression at 10 nM to 10 uM after 24 hrs by luciferase reporter assay | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
| A new avenue toward androgen receptor pan-antagonists: C2 sterically hindered substitution of hydroxy-propanamides. |
AID1569754 | Inhibition of human ERG expressed in CHO cells by whole-cell voltage-clamp analysis | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | A new series of bicalutamide, enzalutamide and enobosarm derivatives carrying pentafluorosulfanyl (SF |
AID711919 | Antagonist activity at AR in human LNCAP cells receptor assessed as inhibition of R1881-induced transcriptional activation at 10 uM by ARE-luciferase reporter gene assay | 2012 | ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6
| Nonsteroidal androgen receptor ligands: versatile syntheses and biological data. |
AID296862 | Inhibition of prostate weight in castrated immature male Sprague-Dawley rat at 2 mg/day relative to control | 2007 | Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16
| Design, synthesis, and in vivo SAR of a novel series of pyrazolines as potent selective androgen receptor modulators. |
AID491348 | Growth inhibition of mouse SC3 cells after 3 days by WST-8 assay | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13
| Design and synthesis of androgen receptor full antagonists bearing a p-carborane cage: promising ligands for anti-androgen withdrawal syndrome. |
AID1416293 | Antiproliferative activity against human LNCAP cells after 96 hrs by propidium iodide staining-based fluorescence assay | 2017 | MedChemComm, Jul-01, Volume: 8, Issue:7
| Rational design and synthesis of novel phenylsulfonyl-benzamides as anti-prostate cancer agents. |
AID731972 | Half life in mouse plasma | 2013 | Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
| Design, synthesis, and biological evaluation of 3-aryl-3-hydroxy-1-phenylpyrrolidine derivatives as novel androgen receptor antagonists. |
AID1313189 | Half life in human liver microsomes at 3 uM in presence of NADPH by LC-MS/MS analysis | 2016 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
| Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety. |
AID694141 | Antagonist activity at wild type human androgen receptor expressed in COS-1 cells co-transfected with pSG5 assessed as testosterone induced luciferase activity at 10 uM after 18 hrs relative untreated control | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| Design, synthesis, and biological evaluation of nonsteroidal cycloalkane[d]isoxazole-containing androgen receptor modulators. |
AID1635256 | Antagonist activity at rat androgen receptor fused with DNA-binding domain of GAL4 expressed in AR-UAS-bla GripTite 293 cells assessed as inhibition of R1881-induced receptor activation at 1000 nM preincubated for 30 mins followed by R1881 addition measur | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID1635245 | Half life in human liver microsomes at 3 uM preincubated with compound followed by NADPH addition by LC-MS/MS analysis | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID1442877 | Antagonist activity at androgen receptor in human LNCAP cells assessed as cell growth inhibition after 144 hrs by SRB assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| 1,4-Substituted Triazoles as Nonsteroidal Anti-Androgens for Prostate Cancer Treatment. |
AID1635262 | Antagonist activity at rat androgen receptor fused with DNA-binding domain of GAL4 expressed in AR-UAS-bla GripTite 293 cells assessed as inhibition of R1881-induced receptor activation at 1 nM preincubated for 30 mins followed by R1881 addition measured | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID491346 | Antagonist activity at human androgen receptor expressed in mouse NIH3T3 cells assessed as inhibition of dihydrotestosterone -induced luciferase transactivation activity at 0.1 nM by ARE-luciferase reporter gene assay | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13
| Design and synthesis of androgen receptor full antagonists bearing a p-carborane cage: promising ligands for anti-androgen withdrawal syndrome. |
AID1430118 | Antagonist activity at AR T877A mutant in human LNCAP cells assessed as inhibition of DHT-induced PSA mRNA level at 5 uM after 24 hrs by SYBR Green dye based qPCR method | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
| Design, synthesis and biological evaluation of 2-(4-phenylthiazol-2-yl) isoindoline-1,3-dione derivatives as anti-prostate cancer agents. |
AID711908 | Cytotoxicity against human LNCAP cells assessed as growth inhibition at 2 to 20 uM after 144 hrs by SRB assay | 2012 | ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6
| Nonsteroidal androgen receptor ligands: versatile syntheses and biological data. |
AID711912 | Growth inhibition in human LNCaP-AR cells after 144 hrs by SRB assay | 2012 | ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6
| Nonsteroidal androgen receptor ligands: versatile syntheses and biological data. |
AID1362958 | Antiproliferative activity against human PC3 cells assessed as inhibition of cell proliferation after 3 days in presence of DHT by WST8 assay | 2018 | Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18
| Structure-activity relationship of novel (benzoylaminophenoxy)phenol derivatives as anti-prostate cancer agents. |
AID280723 | Displacement of [3H]R1881 from rat AR relative to R1881 | 2007 | Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
| Synthesis and biological evaluation of [18F]bicalutamide, 4-[76Br]bromobicalutamide, and 4-[76Br]bromo-thiobicalutamide as non-steroidal androgens for prostate cancer imaging. |
AID1362957 | Antagonist activity at AR H874Y mutant in human 22Rv1 cells assessed as inhibition of DHT-induced cell proliferation measured after 3 days by WST8 assay | 2018 | Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18
| Structure-activity relationship of novel (benzoylaminophenoxy)phenol derivatives as anti-prostate cancer agents. |
AID1635246 | Apparent permeability from apical to basolateral side in human Caco2 cells at 10 uM incubated for 120 mins by LC-MS/MS analysis | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID1187550 | Inhibition of R1881-induced DNA synthesis in human LNCAP cells at 10 to 20 uM after 18 hrs by BrdU incorporation assay | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
| A new avenue toward androgen receptor pan-antagonists: C2 sterically hindered substitution of hydroxy-propanamides. |
AID339523 | Displacement of [3H]testosterone from human recombinant androgen receptor T877A mutant expressed in LNCaP cells | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14
| 4-(Anilino)pyrrole-2-carboxamides: Novel non-steroidal/non-anilide type androgen antagonists effective upon human prostate tumor LNCaP cells with mutated nuclear androgen receptor. |
AID1313188 | Agonist activity at GAL4 DBD-fused androgen receptor LBD (unknown origin) transfected in UAS-bla GripTite 293 cells at 10 uM after 16 to 24 hrs by by beta-lactamase reporter gene assay | 2016 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
| Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety. |
AID1187563 | Inhibition of cell survival in human CWR22Rv1 cells after 144 hrs by TUNEL assay | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
| A new avenue toward androgen receptor pan-antagonists: C2 sterically hindered substitution of hydroxy-propanamides. |
AID1612504 | Induction of full length androgen receptor degradation in human LNCaP cells at 1 uM after 24 hrs in presence of R1881 by Western blot analysis relative to control | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| New Generation of Selective Androgen Receptor Degraders: Our Initial Design, Synthesis, and Biological Evaluation of New Compounds with Enzalutamide-Resistant Prostate Cancer Activity. |
AID1416292 | Antiproliferative activity against human DU145 cells after 96 hrs by propidium iodide staining-based fluorescence assay | 2017 | MedChemComm, Jul-01, Volume: 8, Issue:7
| Rational design and synthesis of novel phenylsulfonyl-benzamides as anti-prostate cancer agents. |
AID298548 | Antagonist efficacy at human androgen receptor assessed as inhibition of DHT activity by luciferase reporter gene assay | 2007 | Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
| Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators. |
AID1635242 | Agonist activity at rat androgen receptor fused with DNA-binding domain of GAL4 expressed in AR-UAS-bla GripTite 293 cells assessed as receptor activation at 10 uM incubated for 16 to 24 hrs by betalactamase reporter gene assay relative to control | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID348771 | Binding affinity to rat androgen receptor by competitive inhibition assay | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
| Effect of B-ring substitution pattern on binding mode of propionamide selective androgen receptor modulators. |
AID298549 | Binding affinity to human AR | 2007 | Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
| Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators. |
AID1612502 | Displacement of [3H]-mibolerone from recombinant wild-type GST-tagged androgen receptor LBD (unknown origin) after 16 hrs by scintillation counting analysis | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| New Generation of Selective Androgen Receptor Degraders: Our Initial Design, Synthesis, and Biological Evaluation of New Compounds with Enzalutamide-Resistant Prostate Cancer Activity. |
AID1430122 | Antagonist activity at AR T877A mutant in human LNCAP cells assessed as inhibition of DHT-induced c-Myc mRNA level at 5 uM after 24 hrs by SYBR Green dye based qPCR method | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
| Design, synthesis and biological evaluation of 2-(4-phenylthiazol-2-yl) isoindoline-1,3-dione derivatives as anti-prostate cancer agents. |
AID491349 | Growth inhibition of human LNCAP cells after 3 days | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13
| Design and synthesis of androgen receptor full antagonists bearing a p-carborane cage: promising ligands for anti-androgen withdrawal syndrome. |
AID39451 | Binding affinity against cytosolic androgen receptor from ventral prostate of rats using [3H]MIB competitive binding assay (relative to dihydro testosterone) | 2004 | Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
| A ligand-based approach to identify quantitative structure-activity relationships for the androgen receptor. |
AID1250206 | Antagonist activity at AR T877A mutant expressed in human LNCaP cells assessed as inhibition of 10 nM testosterone-induced PSA production after 48 hrs by ELISA method | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Design and synthesis of 4-benzyl-1-(2H)-phthalazinone derivatives as novel androgen receptor antagonists. |
AID1635261 | Antagonist activity at rat androgen receptor fused with DNA-binding domain of GAL4 expressed in AR-UAS-bla GripTite 293 cells assessed as inhibition of R1881-induced receptor activation at 3.16 nM preincubated for 30 mins followed by R1881 addition measur | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID339527 | Antiproliferative activity against human LNCaP cells | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14
| 4-(Anilino)pyrrole-2-carboxamides: Novel non-steroidal/non-anilide type androgen antagonists effective upon human prostate tumor LNCaP cells with mutated nuclear androgen receptor. |
AID339517 | Displacement of [3H]testosterone from wild type human androgen receptor | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14
| 4-(Anilino)pyrrole-2-carboxamides: Novel non-steroidal/non-anilide type androgen antagonists effective upon human prostate tumor LNCaP cells with mutated nuclear androgen receptor. |
AID1612503 | Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of R1881-induced receptor transactivation after 24 hrs by luciferase reporter gene assay | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| New Generation of Selective Androgen Receptor Degraders: Our Initial Design, Synthesis, and Biological Evaluation of New Compounds with Enzalutamide-Resistant Prostate Cancer Activity. |
AID1612505 | Induction of androgen receptor splice variant mutant degradation in human 22RV1 cells at 10 uM after 24 hrs in presence of R1881 by Western blot analysis relative to control | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| New Generation of Selective Androgen Receptor Degraders: Our Initial Design, Synthesis, and Biological Evaluation of New Compounds with Enzalutamide-Resistant Prostate Cancer Activity. |
AID239949 | Inhibition of [3H]mibolerone binding to cytosolic androgen receptor of rat ventral prostate | 2005 | Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
| Three-dimensional structure-activity relationships of nonsteroidal ligands in complex with androgen receptor ligand-binding domain. |
AID1430120 | Antagonist activity at AR T877A mutant in human LNCAP cells assessed as inhibition of DHT-induced TMPRSS2 mRNA level at 5 uM after 24 hrs by SYBR Green dye based qPCR method | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
| Design, synthesis and biological evaluation of 2-(4-phenylthiazol-2-yl) isoindoline-1,3-dione derivatives as anti-prostate cancer agents. |
AID1430113 | Selectivity ratio of IC50 for AR negative human PC3 cells to IC50 for AR T877A mutant in human LNCAP cells | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
| Design, synthesis and biological evaluation of 2-(4-phenylthiazol-2-yl) isoindoline-1,3-dione derivatives as anti-prostate cancer agents. |
AID1797839 | Competitive Radioligand Displacement Assay from Article 10.1016/j.bmc.2006.06.019: \\Arylisothiocyanato selective androgen receptor modulators (SARMs) for prostate cancer.\\ | 2006 | Bioorganic & medicinal chemistry, Oct-01, Volume: 14, Issue:19
| Arylisothiocyanato selective androgen receptor modulators (SARMs) for prostate cancer. |
AID1798655 | Competitive Radioligand Displacement Assay from Article 10.1016/j.bmcl.2008.09.002: \\Effect of B-ring substitution pattern on binding mode of propionamide selective androgen receptor modulators.\\ | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
| Effect of B-ring substitution pattern on binding mode of propionamide selective androgen receptor modulators. |
AID1797753 | Competitive Radioligand Displacement Assay and AR-Mediated Transcription Activation Assay from Article 10.1006/bbrc.1998.8209: \\Discovery of nonsteroidal androgens.\\ | 1998 | Biochemical and biophysical research communications, Mar-06, Volume: 244, Issue:1
| Discovery of nonsteroidal androgens. |
AID1797752 | Competitive Radioligand Displacement Assay from Article 10.1021/jm990027x: \\Chiral nonsteroidal affinity ligands for the androgen receptor. 1. Bicalutamide analogues bearing electrophilic groups in the B aromatic ring.\\ | 2000 | Journal of medicinal chemistry, Feb-24, Volume: 43, Issue:4
| Chiral nonsteroidal affinity ligands for the androgen receptor. 1. Bicalutamide analogues bearing electrophilic groups in the B aromatic ring. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |