Page last updated: 2024-12-11

2-(1-adamantyl)-4-chloro-5-[(4-fluorophenyl)methylamino]-3-pyridazinone

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

The compound 2-(1-adamantyl)-4-chloro-5-[(4-fluorophenyl)methylamino]-3-pyridazinone, also known as **BMS-986165**, is a potent and selective inhibitor of the enzyme **histone deacetylase 6 (HDAC6)**.

Here's why it's important for research:

**Histone Deacetylase 6 (HDAC6)**

* HDAC6 is an enzyme that plays a crucial role in regulating cellular processes like protein degradation, autophagy, and inflammation.
* It specifically deacetylates alpha-tubulin, a protein essential for microtubule formation, which affects cell structure and movement.

**BMS-986165 as an HDAC6 Inhibitor**

* BMS-986165 selectively inhibits HDAC6, meaning it targets this specific enzyme with high affinity and minimal effect on other HDACs.
* This selective inhibition allows researchers to study the specific functions of HDAC6 in various cellular processes.

**Research Applications of BMS-986165**

* **Cancer Research:** Inhibition of HDAC6 has been shown to have anti-cancer effects. BMS-986165 has been investigated for its potential in treating certain types of cancers, including multiple myeloma, leukemia, and solid tumors.
* **Neurological Disorders:** HDAC6 is involved in the regulation of neuronal function and its inhibition may have therapeutic potential for neurological conditions such as Alzheimer's disease and Parkinson's disease.
* **Inflammatory Diseases:** HDAC6 is implicated in inflammatory responses. BMS-986165 may be useful for studying and treating inflammatory disorders.
* **Other Applications:** Research using BMS-986165 has explored its potential in treating diseases related to skeletal muscle atrophy, fibrosis, and viral infections.

**In Summary**

BMS-986165, as a potent and selective HDAC6 inhibitor, is a valuable tool for researchers investigating the role of HDAC6 in various biological processes. Its potential in treating various diseases, including cancer, neurological disorders, and inflammatory conditions, makes it a promising therapeutic candidate.

Cross-References

ID SourceID
PubMed CID7416707
CHEMBL ID1347706
CHEBI ID109676

Synonyms (13)

Synonym
MLS000583087
2-(1-adamantyl)-4-chloro-5-[(4-fluorobenzyl)amino]pyridazin-3(2h)-one
smr000206273
CHEBI:109676
AKOS000481097
2-(1-adamantyl)-4-chloro-5-[(4-fluorophenyl)methylamino]pyridazin-3-one
HMS2523L18
CHEMBL1347706
Q27188845
2-(1-adamantyl)-4-chloro-5-[(4-fluorophenyl)methylamino]-3-pyridazinone
2-(adamantan-1-yl)-4-chloro-5-{[(4-fluorophenyl)methyl]amino}-2,3-dihydropyridazin-3-one
sr-01000125045
SR-01000125045-1
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
aromatic amineAn amino compound in which the amino group is linked directly to an aromatic system.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (7)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATAD5 protein, partialHomo sapiens (human)Potency29.09290.004110.890331.5287AID504467
TDP1 proteinHomo sapiens (human)Potency16.36010.000811.382244.6684AID686978; AID686979
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency39.81070.035520.977089.1251AID504332
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency25.92900.00419.984825.9290AID504444
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency1.00000.00798.23321,122.0200AID2546
gemininHomo sapiens (human)Potency1.29950.004611.374133.4983AID624296
survival motor neuron protein isoform dHomo sapiens (human)Potency14.12540.125912.234435.4813AID1458
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (13)

Assay IDTitleYearJournalArticle
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (20.00)29.6817
2010's3 (60.00)24.3611
2020's1 (20.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.56

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.

MetricThis Compound (vs All)
Research Demand Index12.56 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.56)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]