| ID Source | ID |
|---|---|
| PubMed CID | 49830252 |
| CHEMBL ID | 4471178 |
| SCHEMBL ID | 22789735 |
| MeSH ID | M0555912 |
| Synonym |
|---|
| LONGDAYSIN , |
| 9-isopropyl-n-(3-(trifluoromethyl)benzyl)-9h-purin-6-amine , |
| S6578 |
| c16h16f3n5 |
| CHEMBL4471178 , |
| longdaysin, >=98% (hplc) |
| BS-15249 |
| mfcd20527323 |
| BCP32583 |
| 1353867-91-0 |
| CS-0007385 |
| 9-propan-2-yl-n-[[3-(trifluoromethyl)phenyl]methyl]purin-6-amine |
| D81043 |
| NCGC00487170-01 |
| HY-18285 |
| AKOS037515668 |
| bdbm50531922 |
| SCHEMBL22789735 |
| reksfccydqmsin-uhfffaoysa-n |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Longdaysin was amenable for chemical modification to perform affinity chromatography coupled with mass spectrometry analysis to identify target proteins." | ( High-throughput chemical screen identifies a novel potent modulator of cellular circadian rhythms and reveals CKIα as a clock regulatory kinase. Breton, G; Etchegaray, JP; Garcia, M; Hirota, T; Kay, SA; Lee, JW; Lewis, WG; Liu, X; Peters, EC; Schultz, PG; Traver, D; Zhang, EE, 2010) | 1.08 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Longdaysin treatment inhibited PER1 degradation, providing insight into the mechanism of longdaysin-dependent period lengthening." | ( High-throughput chemical screen identifies a novel potent modulator of cellular circadian rhythms and reveals CKIα as a clock regulatory kinase. Breton, G; Etchegaray, JP; Garcia, M; Hirota, T; Kay, SA; Lee, JW; Lewis, WG; Liu, X; Peters, EC; Schultz, PG; Traver, D; Zhang, EE, 2010) | 1.08 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "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 | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Cyclin-dependent kinase 2 | Homo sapiens (human) | IC50 (µMol) | 13.0000 | 0.0004 | 1.0444 | 10.0000 | AID1624556 |
| Mitogen-activated protein kinase 1 | Homo sapiens (human) | IC50 (µMol) | 59.0000 | 0.0003 | 1.6878 | 9.2000 | AID1624559 |
| Mitogen-activated protein kinase 8 | Homo sapiens (human) | IC50 (µMol) | 92.0000 | 0.0020 | 1.0173 | 5.4200 | AID1624560 |
| Casein kinase I isoform alpha | Homo sapiens (human) | IC50 (µMol) | 12.0000 | 0.0010 | 2.2499 | 10.0000 | AID1624555 |
| Casein kinase I isoform delta | Homo sapiens (human) | IC50 (µMol) | 12.0000 | 0.0040 | 1.1272 | 10.0000 | AID1624557 |
| Cyclin-dependent kinase 7 | Homo sapiens (human) | IC50 (µMol) | 32.0000 | 0.0001 | 0.9106 | 9.2000 | AID1624558 |
| Cyclin-H | Homo sapiens (human) | IC50 (µMol) | 32.0000 | 0.0005 | 1.0823 | 9.2000 | AID1624558 |
| CDK-activating kinase assembly factor MAT1 | Homo sapiens (human) | IC50 (µMol) | 32.0000 | 0.0030 | 1.6892 | 9.2000 | AID1624558 |
| [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) |
|---|---|---|---|---|---|---|---|
| Casein kinase I isoform alpha | Homo sapiens (human) | EC (µMol) | 1.8950 | 0.3900 | 3.4375 | 9.0000 | AID1624534; AID1624535 |
| Casein kinase I isoform delta | Homo sapiens (human) | EC (µMol) | 1.8950 | 0.3900 | 3.4375 | 9.0000 | AID1624534; AID1624535 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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. |
| 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. |
| AID1624540 | Inhibition of N-terminal GST-tagged recombinant full-length human MAPK1 expressed in Escherichia coli at 5 uM using MBP as substrate after 3 hrs by kinase-glo luminescent assay relative to control | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase Iα and δ. |
| AID1624559 | Inhibition of N-terminal GST-tagged recombinant full-length human MAPK1 expressed in Escherichia coli using MBP1 as substrate after 3 hrs by kinase-glo luminescent assay relative to control | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase Iα and δ. |
| AID1624555 | Inhibition of recombinant full length human GST-tagged CK1apha expressed in baculovirus using peptide as substrate after 3 hrs by kinase-glo luminescent assay | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase Iα and δ. |
| AID1624560 | Inhibition of MAPK8 (unknown origin) using peptide as substrate after 3 hrs by kinase-glo luminescent assay relative to control | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase Iα and δ. |
| AID1624534 | Inhibition of CK1alpha/CK1delta in human U2OS cells co-expressing Bmal1-dLuc assessed as modulation circadian clock by measuring drug level causing 1 hr circadian period lengthening measured every 100 mins by luminescence assay | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase Iα and δ. |
| AID1624550 | Modulation of circadian rhythms in C57BL/6J mouse assessed as lengthening of time period of circadian behavior at 1 mM administered via infusion using osmotic pump by passive infrared sensor analysis | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase Iα and δ. |
| AID1624551 | Modulation of circadian rhythms in C57BL/6J mouse assessed as lengthening of time period of circadian behavior at 3 mM administered via infusion using osmotic pump by passive infrared sensor analysis | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase Iα and δ. |
| AID1624535 | Inhibition of CK1alpha/CK1delta in human U2OS cells co-expressing Bmal1-dLuc assessed as modulation circadian clock by measuring drug level causing 5 hrs circadian period lengthening measured every 100 mins by luminescence assay | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase Iα and δ. |
| AID1624539 | Inhibition of recombinant full length C-terminal human His-tagged CDK7/cyclin H/N-terminal MAT1 expressed in baculovirus expression system at 5 uM using Cdk7/9 peptide as substrate after 3 hrs by kinase-glo luminescent assay relative to control | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase Iα and δ. |
| AID1624553 | Modulation of circadian rhythms in C57BL/6J mouse assessed as lengthening of time period of circadian behavior at 15 mM administered via infusion using osmotic pump by passive infrared sensor analysis | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase Iα and δ. |
| AID1624557 | Inhibition of recombinant N-terminal human GST-tagged CK1delta (1 to 294 residues) expressed in Escherichia coli using RKKKAEpSVASLTSQCSYSS peptide as substrate after 3 hrs by kinase-glo luminescent assay relative to control | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase Iα and δ. |
| AID1624538 | Inhibition of CDK2 (unknown origin) at 5 uM after 3 hrs by kinase-glo luminescent assay relative to control | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase Iα and δ. |
| AID1624536 | Inhibition of recombinant full length human GST-tagged CK1apha expressed in baculovirus at 5 uM using peptide as substrate after 3 hrs by kinase-glo luminescent assay | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase Iα and δ. |
| AID1624552 | Modulation of circadian rhythms in C57BL/6J mouse assessed as lengthening of time period of circadian behavior at 5 mM administered via infusion using osmotic pump by passive infrared sensor analysis | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase Iα and δ. |
| AID1624558 | Inhibition of recombinant full length C-terminal human His-tagged CDK7/cyclin H/N-terminal MAT1 expressed in baculovirus expression system using Cdk7/9 peptide as substrate after 3 hrs by kinase-glo luminescent assay relative to control | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase Iα and δ. |
| AID1624556 | Inhibition of CDK2 (unknown origin) after 3 hrs by kinase-glo luminescent assay relative to control | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase Iα and δ. |
| AID1624537 | Inhibition of recombinant N-terminal human GST-tagged CK1delta (1 to 294 residues) expressed in Escherichia coli at 5 uM using RKKKAEpSVASLTSQCSYSS peptide as substrate after 3 hrs by kinase-glo luminescent assay relative to control | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase Iα and δ. |
| [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 | 8 (100.00) | 24.3611 |
| 2020's | 0 (0.00) | 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 moderate demand-to-supply ratio for research on this compound.
| This Compound (23.82) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 8 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||