| ID Source | ID |
|---|---|
| PubMed CID | 9819086 |
| CHEMBL ID | 2447887 |
| SCHEMBL ID | 996941 |
| MeSH ID | M0395380 |
| Synonym |
|---|
| 1-(2,4-dichlorobenzyl)-1h-indazole-3-carbohydrazide |
| adjudin , |
| 1-[(2,4-dichlorophenyl)methyl]indazole-3-carbohydrazide |
| S0454 |
| CHEMBL2447887 |
| CS-5125 |
| HY-18996 |
| SCHEMBL996941 |
| AC-35357 |
| 252025-52-8 |
| FT-0697002 |
| DTXSID0040383 |
| af-2364 |
| af 2364 |
| AKOS026750513 |
| c15h12cl2n4o |
| NCGC00484074-01 |
| adjudin (af-2364) |
| Q4683181 |
| EX-A2468 |
| BS-16318 |
| af-2364;af 2364;af2364 |
| BCP13328 |
| 1-((2,4-dichlorophenyl)methyl)indazole-3-carbohydrazide |
| 1-((2,4-dichlorophenyl)methyl)-1h-indazole-3-carboxylic acid hydrazide |
| 1h-indazole-3-carboxylic acid, 1-((2,4-dichlorophenyl)methyl)-, hydrazide |
| VZT8V72829 , |
| 1h-indazole-3-carboxylic acid, 1-[(2,4-dichlorophenyl)methyl]-, hydrazide |
| 1-(2,4-dichlorobenzyl)indazole-3-carbohydrazide |
| F85301 |
| 1-(2,4-dichlorobenzyl)-indazole-3-carbohydrazide |
| A877667 |
| unii-vzt8v72829 |
| 1-(2,4-dichloro-benzyl)-1h-indazole-3-carboxylic acid hydrazide |
| CKA02552 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " These data have clearly illustrated the low bioavailability of AF-2364 in rats and that this compound is not specifically taken up by any organs including the testis or the epididymis." | ( AF-2364 [1-(2,4-dichlorobenzyl)-1H-indazole-3-carbohydrazide] is a potential male contraceptive: a review of recent data. Bonanomi, M; Cheng, CY; Lee, NP; Lui, WY; Mo, MY; Mruk, D; Silvestrini, B; Siu, MK; Wong, CH, 2005) | 0.33 |
| " Intravenous treatment showed a more severe disturbance of spermatogenesis compared with gavage treatment, which was correlated with bioavailability of the drug." | ( Adjudin targeting rabbit germ cell adhesion as a male contraceptive: a pharmacokinetics study. Bonanomi, M; Chen, BB; Chen, GR; Cheng, CY; Ge, RS; Hu, GX; Hu, LF; Li, JW; Mruk, DD; Silvestrini, B; Yang, DZ, ) | 0.13 |
| " For instance, adjudin, 1-(2,4-dichlorobenzyl)-1H-indazole-3-carbohydrazide, a potential nonhormonal male contraceptive that exerts its effects on germ cell adhesion, most notably at the Sertoli cell-spermatid interface, to induce "premature" germ cell loss from the seminiferous epithelium mimicking spermiation, has a relatively poor bioavailability largely because of the BTB." | ( Role of P-glycoprotein at the blood-testis barrier on adjudin distribution in the testis: a revisit of recent data. Bonanomi, M; Cheng, CY; Cheng, YH; Jenardhanan, P; Mathur, PP; Mok, KW; Mruk, DD; Silvestrini, B; Su, L, 2012) | 0.38 |
| "Drug transporters determine the bioavailability of drugs in the testis behind the blood-testis barrier (BTB)." | ( Breast cancer resistance protein regulates apical ectoplasmic specialization dynamics stage specifically in the rat testis. Cheng, CY; Mruk, DD; Qian, X; Wong, EW, 2013) | 0.39 |
| " Herein, we summarize recent findings pertinent to adjudin, a non-hormonal male contraceptive, and molecular interactions of adjudin with BCRP so that this information can be helpful to devise delivery strategies to evade BCRP in the tunica propria to improve its bioavailability in the testis." | ( Interaction of oligomeric breast cancer resistant protein (BCRP) with adjudin: a male contraceptive with anti-cancer activity. Cheng, CY; Cheng, YH; Jenardhanan, P; Mathur, PP; Qian, X; Silvestrini, B; Xia, W, 2014) | 0.4 |
| " Recent advances in drug formulations, such as drug particle micronization (<50 μm) and co-grinding of drug particles with ß-cyclodextrin have improved bioavailability of contraceptives via considerable increase in solubility." | ( Effective Delivery of Male Contraceptives Behind the Blood-Testis Barrier (BTB) - Lesson from Adjudin. Bonanomi, M; Chen, H; Cheng, CY; Mruk, DD; Silvestrini, B; Xia, W, 2016) | 0.43 |
| "The bioavailability of the non-hormonal male contraceptive adjudin is low in rats due to the blood-testis barrier (BTB)." | ( F5-peptide enhances the efficacy of the non-hormonal male contraceptive adjudin. Chen, H; Cheng, CY; Mruk, D; Silvestrini, B; Wong, CKC, 2019) | 0.51 |
| "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 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " Depending on the dosing of the administered compound, rats became infertile for 4-14 wk before their fertility gradually bounced back, illustrating the reversibility and efficacy of these new compounds." | ( Two new male contraceptives exert their effects by depleting germ cells prematurely from the testis. Cheng, CY; Grima, J; Johansson, E; Leone, MG; Mo , MY; Mruk, D; Palmery, M; Saso, L; Silvestrini, B; Zhu , LJ, 2001) | 0.31 |
| " Similarly, oral dosing of WIN 18,446, which inhibits testicular retinoic acid biosynthesis, effectively contracepts rabbits." | ( New approaches to male non-hormonal contraception. Amory, JK; Nya-Ngatchou, JJ, 2013) | 0.39 |
| " This can also reduce long-term toxicity and health risk if the effective dosing can be lowered in order to widen the margin between its safety and efficacy." | ( Role of P-glycoprotein at the blood-testis barrier on adjudin distribution in the testis: a revisit of recent data. Bonanomi, M; Cheng, CY; Cheng, YH; Jenardhanan, P; Mathur, PP; Mok, KW; Mruk, DD; Silvestrini, B; Su, L, 2012) | 0.38 |
| 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. |
| 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. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| 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. |
| [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 | 24 (34.29) | 29.6817 |
| 2010's | 38 (54.29) | 24.3611 |
| 2020's | 8 (11.43) | 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 weak demand-to-supply ratio for research on this compound.
| This Compound (10.35) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 13 (17.57%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 61 (82.43%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||