| ID Source | ID |
|---|---|
| PubMed CID | 24872560 |
| CHEMBL ID | 3183409 |
| SCHEMBL ID | 909297 |
| MeSH ID | M0573548 |
| Synonym |
|---|
| apalutamide , |
| HY-16060 |
| arn 509 |
| unii-4t36h88ua7 |
| 4t36h88ua7 , |
| jnj 56021927 |
| 4-(7-(6-cyano-5-(trifluoromethyl)pyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro(3.4)octan-5-yl)-2-fluoro-n-methylbenzamide |
| apalutamide [inn] |
| arn509 |
| jnj-56021927 |
| arn-509 |
| NCGC00346725-01 |
| PB27306 |
| CS-0885 |
| S2840 |
| 956104-40-8 |
| MLS006011109 |
| smr004702891 |
| 4-(7-(6-cyano-5-(trifluoromethyl)pyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]octan-5-yl)-2-fluoro-n-methylbenzamide |
| apalutamide [orange book] |
| benzamide, 4-(7-(6-cyano-5-(trifluoromethyl)-3-pyridinyl)-8-oxo-6-thioxo-5,7-diazaspiro(3.4)oct-5-yl)-2-fluoro-n-methyl- |
| apalutamide [mi] |
| erleada |
| apalutamide [who-dd] |
| apalutamide [jan] |
| bdbm50094975 |
| SCHEMBL909297 |
| AC-27403 |
| CHEMBL3183409 |
| gtpl9043 |
| 4-[7-[6-cyano-5-(trifluoromethyl)pyridin-3-yl]-8-oxo-6-sulfanylidene-5,7-diazaspiro[3.4]octan-5-yl]-2-fluoro-n-methylbenzamide |
| AKOS025401932 |
| J-519596 |
| DTXSID40241899 , |
| EX-A089 |
| HMS3656N12 |
| mfcd22380626 |
| NCGC00346725-06 |
| ar509 |
| 4-{7-[6-cyano-5-(trifluoromethyl)pyridin-3-yl]-8-oxo-6-sulfanylidene-5,7-diazaspiro[3.4]octan-5-yl}-2-fluoro-n-methylbenzamide |
| SW220300-1 |
| apalutamidearn509 |
| DB11901 |
| BCP05829 |
| ar509/ar-509 |
| 956104-40-8 (free base) |
| apalutamide (arn-509) |
| 24872560, erleada, c21h15f4n5o2s |
| AS-35181 |
| Q21098975 |
| D11040 |
| erleada (tn) |
| apalutamide (jan/inn) |
| AMY24182 |
| CCG-264760 |
| nsc-771649 |
| nsc771649 |
| nsc-794776 |
| nsc794776 |
| NCGC00346725-02 |
| EN300-18167004 |
| apalutamida |
| dtxcid20164390 |
| l02bb05 |
| apalutamidum |
| Z2037280438 |
Apalutamide (APA) is a next-generation androgen receptor antagonist for the treatment of advanced prostate cancer. Apalutamide is a novel androgen signalling inhibitor developed to be used in combination with continuous androgen deprivation therapy (ADT)
Apalutamide + ADT treatment was efficacious in extending rPFS and OS. Treatment with apalutamide plus AA-P was well tolerated and showed evidence of antitumor activity.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Apalutamide + ADT treatment was efficacious in extending rPFS and OS versus placebo + ADT. " | ( Efficacy and safety exposure-response relationships of apalutamide in patients with metastatic castration-sensitive prostate cancer: results from the phase 3 TITAN study. Ackaert, O; Agarwal, N; Chi, K; Chien, C; Chowdhury, S; Karsh, L; Lopez-Gitlitz, A; McCarthy, S; Ruixo, CP; Ruixo, JP; T'jollyn, H, 2022) | 2.41 |
| "Treatment with apalutamide plus AA-P was well tolerated and showed evidence of antitumor activity in patients with mCRPC, including those with disease progression on AR signaling inhibitors. " | ( Pharmacokinetics, Safety, and Antitumor Effect of Apalutamide with Abiraterone Acetate plus Prednisone in Metastatic Castration-Resistant Prostate Cancer: Phase Ib Study. Abrams, C; Attard, G; Chi, KN; Chien, C; de Jonge, MJA; de Wit, R; Friedlander, TW; Hellemans, P; Jiao, JJ; Posadas, EM; Saad, F; Yu, MK, 2020) | 1.16 |
Nearly half of the Japanese patients in this study experienced skin adverse events following apalutamide administration. A lower body weight is a significant risk factor for these adverse events. The onset is within 6 months of initiation of therapy.
A population pharmacokinetic modelling approach was successfully applied to describe the pharmacokinetics of apalutamide and N-desmethyl-apalutamides. No clinically significant pharmacokeretic interaction was observed between abiraterone and apalUTamide; however, apalutsamide decreased exposure to prednisone.
Two phase I studies assessed the drug-drug interaction potential of apalutamide.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Two phase I studies assessed the drug-drug interaction potential of apalutamide as a substrate and perpetrator." | ( Pharmacokinetic Drug-Drug Interaction of Apalutamide, Part 1: Clinical Studies in Healthy Men and Patients with Castration-Resistant Prostate Cancer. Armas, D; Bulat, I; Carles, J; Chien, C; Duran, I; Hellemans, P; Jiao, J; Mitselos, A; Ward, P, 2020) | 1.06 |
| "We aimed to predict CYP3A4 and CYP2C8 inhibitor/inducer effects on the steady-state pharmacokinetics of apalutamide and total potency-adjusted pharmacologically active moieties, and simulated drug-drug interaction (DDI) between single-dose and repeated-dose apalutamide coadministered with known inhibitors/inducers." | ( Pharmacokinetic Drug-Drug Interaction of Apalutamide, Part 2: Investigating Interaction Potential Using a Physiologically Based Pharmacokinetic Model. Chien, C; De Zwart, L; Lopez-Gitlitz, A; Monshouwer, M; Ouellet, D; Snoeys, J; Van den Bergh, A; Ward, P, 2020) | 1.04 |
| " Therefore, we investigated the characteristics of autophagic response to ARN-509 treatment and evaluated the potential effect of a combination with autophagy inhibition." | ( Apalutamide in combination with autophagy inhibitors improves treatment effects in prostate cancer cells. Eberli, D; Kranzbühler, B; Mortezavi, A; Salemi, S; Sulser, T, 2020) | 2 |
| " Cells were treated with ARN-509 (50 µM) alone or in combination with the autophagy inhibitors 3-methyladenine (3MA, 5 mM) or chloroquine (Chl, 20 µM) or with ATG5 siRNA knock-down." | ( Apalutamide in combination with autophagy inhibitors improves treatment effects in prostate cancer cells. Eberli, D; Kranzbühler, B; Mortezavi, A; Salemi, S; Sulser, T, 2020) | 2 |
| " Furthermore, in combination with autophagy inhibitors, ARN-509 provided a significantly elevated antitumor effect, thus providing a new therapeutic approach potentially translatable to patients." | ( Apalutamide in combination with autophagy inhibitors improves treatment effects in prostate cancer cells. Eberli, D; Kranzbühler, B; Mortezavi, A; Salemi, S; Sulser, T, 2020) | 2 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "In this phase 1 study, the absolute bioavailability and absorption, metabolism, and excretion (AME) of apalutamide, a competitive inhibitor of the androgen receptor, were evaluated in 12 healthy men." | ( Apalutamide Absorption, Metabolism, and Excretion in Healthy Men, and Enzyme Reaction in Human Hepatocytes. Chien, C; Cuyckens, F; de Vries, R; Jacobs, F; Mannens, G; Snoeys, J; Ward, P, 2019) | 2.17 |
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 18.9991 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 5.1998 | 0.0013 | 10.1577 | 42.8575 | AID1259252; AID1259253; AID1259255; AID1259256 |
| G | Vesicular stomatitis virus | Potency | 6.7412 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Interferon beta | Homo sapiens (human) | Potency | 6.7412 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 6.7412 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 6.7412 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 6.7412 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Gamma-aminobutyric acid receptor subunit pi | Homo sapiens (human) | IC50 (µMol) | 3.0000 | 0.0001 | 1.0201 | 6.0000 | AID1885098 |
| Gamma-aminobutyric acid receptor subunit delta | Homo sapiens (human) | IC50 (µMol) | 3.0000 | 0.0001 | 1.0201 | 6.0000 | AID1885098 |
| Androgen receptor | Homo sapiens (human) | IC50 (µMol) | 0.0981 | 0.0000 | 0.8753 | 10.0000 | AID1466853; AID1612503; AID1681923; AID1705455 |
| Androgen receptor | Homo sapiens (human) | Ki | 0.5266 | 0.0002 | 0.4240 | 7.2000 | AID1233505; AID1612502; AID1705455 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Homo sapiens (human) | IC50 (µMol) | 3.0000 | 0.0001 | 1.1494 | 8.0000 | AID1885098 |
| Androgen receptor | Rattus norvegicus (Norway rat) | Ki | 1.4520 | 0.0003 | 1.2185 | 8.9270 | AID1681924 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Homo sapiens (human) | IC50 (µMol) | 3.0000 | 0.0001 | 1.0393 | 6.0000 | AID1885098 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Homo sapiens (human) | IC50 (µMol) | 3.0000 | 0.0001 | 1.2915 | 8.0000 | AID1885098 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Homo sapiens (human) | IC50 (µMol) | 3.0000 | 0.0001 | 1.3018 | 8.0000 | AID1885098 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Homo sapiens (human) | IC50 (µMol) | 3.0000 | 0.0001 | 0.9800 | 6.0000 | AID1885098 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Homo sapiens (human) | IC50 (µMol) | 3.0000 | 0.0001 | 1.1993 | 6.0000 | AID1885098 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Homo sapiens (human) | IC50 (µMol) | 3.0000 | 0.0001 | 1.0201 | 6.0000 | AID1885098 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Homo sapiens (human) | IC50 (µMol) | 3.0000 | 0.0001 | 0.9374 | 6.0000 | AID1885098 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Homo sapiens (human) | IC50 (µMol) | 3.0000 | 0.0001 | 1.0193 | 6.0000 | AID1885098 |
| Gamma-aminobutyric acid receptor subunit epsilon | Homo sapiens (human) | IC50 (µMol) | 3.0000 | 0.0001 | 1.0201 | 6.0000 | AID1885098 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Homo sapiens (human) | IC50 (µMol) | 3.0000 | 0.0001 | 1.0201 | 6.0000 | AID1885098 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Homo sapiens (human) | IC50 (µMol) | 3.0000 | 0.0001 | 1.0201 | 6.0000 | AID1885098 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Homo sapiens (human) | IC50 (µMol) | 3.0000 | 0.0001 | 1.0201 | 6.0000 | AID1885098 |
| Gamma-aminobutyric acid receptor subunit theta | Homo sapiens (human) | IC50 (µMol) | 3.0000 | 0.0001 | 1.0201 | 6.0000 | AID1885098 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| 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. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1466849 | Cmax in Sprague-Dawley rat at 10 mg/kg administered orally measured up to 24 hrs by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Design, synthesis, and biological evaluation of deuterated apalutamide with improved pharmacokinetic profiles. |
| AID1681924 | Displacement of [3H]-MIB from wild-type rat AR LBD measured after 16 hrs by scintillation counting method | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Pyrazol-1-yl-propanamides as SARD and Pan-Antagonists for the Treatment of Enzalutamide-Resistant Prostate Cancer. |
| AID1466853 | Displacement of [3H]-R1881 from AR in human LNCaP cells preincubated for 30 mins followed by [3H]-R1881 addition measured after 30 mins by microbeta scintillation counter method | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Design, synthesis, and biological evaluation of deuterated apalutamide with improved pharmacokinetic profiles. |
| AID1466844 | Tmax in Balb/c mouse at 10 mg/kg administered orally measured up to 24 hrs by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Design, synthesis, and biological evaluation of deuterated apalutamide with improved pharmacokinetic profiles. |
| AID1233504 | Antiproliferative activity against human LNCAP cells after 3 days | 2015 | European journal of medicinal chemistry, Jun-24, Volume: 99 | Design, synthesis and biological evaluation of novel 5-oxo-2-thioxoimidazolidine derivatives as potent androgen receptor antagonists. |
| AID1833855 | Antagonist activity at human androgen receptor N756A mutant at 10 uM by dual-Glo luciferase assay | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | Discovery of a Novel Androgen Receptor Antagonist Manifesting Evidence to Disrupt the Dimerization of the Ligand-Binding Domain via Attenuating the Hydrogen-Bonding Network Between the Two Monomers. |
| AID1466846 | AUC (0 to 24 hrs) in Balb/c mouse at 10 mg/kg administered orally measured up to 24 hrs by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Design, synthesis, and biological evaluation of deuterated apalutamide with improved pharmacokinetic profiles. |
| 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. |
| AID1466845 | Cmax in Balb/c mouse at 10 mg/kg administered orally measured up to 24 hrs by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Design, synthesis, and biological evaluation of deuterated apalutamide with improved pharmacokinetic profiles. |
| AID1466850 | AUC (0 to infinity) in Sprague-Dawley rat at 10 mg/kg administered orally measured up to 24 hrs by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Design, synthesis, and biological evaluation of deuterated apalutamide with improved pharmacokinetic profiles. |
| AID1466852 | Half life in Sprague-Dawley rat 10 mg/kg administered orally measured up to 24 hrs by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Design, synthesis, and biological evaluation of deuterated apalutamide with improved pharmacokinetic profiles. |
| AID1233505 | Antagonist activity at androgen receptor (unknown origin) | 2015 | European journal of medicinal chemistry, Jun-24, Volume: 99 | Design, synthesis and biological evaluation of novel 5-oxo-2-thioxoimidazolidine derivatives as potent androgen receptor antagonists. |
| AID1466848 | Tmax in Sprague-Dawley rat at 10 mg/kg administered orally measured up to 24 hrs by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Design, synthesis, and biological evaluation of deuterated apalutamide with improved pharmacokinetic profiles. |
| AID1466851 | Mean residence time in Sprague-Dawley rat 10 mg/kg administered orally measured up to 24 hrs by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Design, synthesis, and biological evaluation of deuterated apalutamide with improved pharmacokinetic profiles. |
| AID1681923 | Antagonist activity at recombinant human AR expressed in HEK293 cells assessed as inhibition of R1881-induced transcriptional activity measured after 24 hrs by dual luciferase reporter gene assay | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Pyrazol-1-yl-propanamides as SARD and Pan-Antagonists for the Treatment of Enzalutamide-Resistant Prostate Cancer. |
| AID1705455 | Inhibition of androgen receptor (unknown origin) | 2020 | European journal of medicinal chemistry, Nov-01, Volume: 205 | New drug approvals for 2019: Synthesis and clinical applications. |
| AID1885098 | Binding affinity to GABA A receptor (unknown origin) | 2022 | Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13 | Therapeutic Strategies to Target the Androgen Receptor. |
| 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. |
| AID1466847 | Half life in Balb/c mouse at 10 mg/kg administered orally measured up to 24 hrs by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Design, synthesis, and biological evaluation of deuterated apalutamide with improved pharmacokinetic profiles. |
| 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. |
| AID1346888 | Human Androgen receptor (3C. 3-Ketosteroid receptors) | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7 | Structure-activity relationship for thiohydantoin androgen receptor antagonists for castration-resistant prostate cancer (CRPC). |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| 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 | 72 (34.78) | 24.3611 |
| 2020's | 135 (65.22) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (81.99) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 46 (21.60%) | 5.53% |
| Reviews | 54 (25.35%) | 6.00% |
| Case Studies | 6 (2.82%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 107 (50.23%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||