olomoucine II: structure in first source
ID Source | ID |
---|---|
PubMed CID | 5494414 |
CHEMBL ID | 1094304 |
SCHEMBL ID | 786673 |
MeSH ID | M0451670 |
Synonym |
---|
CK9 , |
DB04662 |
olomoucine ii |
HMS3229J03 |
2-[[[2-[[(2r)-1-hydroxybutan-2-yl]amino]-9-propan-2-ylpurin-6-yl]amino]methyl]phenol |
CHEMBL1094304 |
bdbm50366800 |
2A0C |
SCHEMBL786673 |
AKOS027322559 |
2-{[(2-{[(2r)-1-hydroxybutan-2-yl]amino}-9-(propan-2-yl)-9h-purin-6-yl)amino]methyl}phenol |
nsc 736738 |
2-{[(2-{[(1r)-1-(hydroxymethyl)propyl]amino}-9-isopropyl-9h-purin-6-yl)amino]methyl}phenol |
2-({[2-{[(1r)-1-(hydroxymethyl)propyl]amino}-9-(1-methylethyl)-9h-purin-6-yl]amino}methyl)phenol |
(r)-2-(((2-((1-hydroxybutan-2-yl)amino)-9-isopropyl-9h-purin-6-yl)amino)methyl)phenol |
Q27095411 |
Olomoucine II is a cyclin-dependent kinase inhibitor and a potential antineoplastic agent. It can arrest animal cell cycles.
Excerpt | Reference | Relevance |
---|---|---|
"Olomoucine II is a cyclin-dependent kinase inhibitor and a potential antineoplastic agent because it can arrest animal cell cycles. " | ( Interactions of olomoucine II with human liver microsomal cytochromes P450. Anzenbacher, P; Anzenbacherova, E; Dolezal, K; Popa, I; Siller, M; Strnad, M, 2009) | 2.14 |
Excerpt | Reference | Relevance |
---|---|---|
"Olomoucine II treatment significantly increased the G1 phase cell numbers, decreased the S phase cell numbers, and inhibited DNA replication in mESCs." | ( Cdk2 inhibition prolongs G1 phase progression in mouse embryonic stem cells. Calabkova, L; Divoky, V; Dolezel, P; Kafkova, LR; Koledova, Z; Krystof, V, 2010) | 1.08 |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Cyclin-T1 | Homo sapiens (human) | IC50 (µMol) | 0.8150 | 0.0010 | 0.5585 | 8.0000 | AID738800 |
G2/mitotic-specific cyclin-B2 | Homo sapiens (human) | IC50 (µMol) | 0.0200 | 0.0025 | 1.8172 | 10.0000 | AID53346 |
Cyclin-dependent kinase 1 | Homo sapiens (human) | IC50 (µMol) | 0.0200 | 0.0004 | 1.3452 | 10.0000 | AID53346 |
G2/mitotic-specific cyclin-B1 | Homo sapiens (human) | IC50 (µMol) | 0.0200 | 0.0013 | 1.4518 | 10.0000 | AID53346 |
G1/S-specific cyclin-E1 | Homo sapiens (human) | IC50 (µMol) | 0.0500 | 0.0010 | 1.0404 | 10.0000 | AID738809 |
Cyclin-dependent kinase 2 | Homo sapiens (human) | IC50 (µMol) | 0.0500 | 0.0004 | 1.0444 | 10.0000 | AID738809 |
Cyclin-dependent kinase 9 | Homo sapiens (human) | IC50 (µMol) | 0.8150 | 0.0010 | 0.6236 | 8.0000 | AID738800 |
Cyclin-dependent-like kinase 5 | Homo sapiens (human) | IC50 (µMol) | 0.2700 | 0.0002 | 1.1832 | 10.0000 | AID738802 |
Cyclin-dependent kinase 5 activator 1 | Homo sapiens (human) | IC50 (µMol) | 0.2700 | 0.0010 | 1.2898 | 10.0000 | AID738802 |
G2/mitotic-specific cyclin-B3 | Homo sapiens (human) | IC50 (µMol) | 0.0200 | 0.0025 | 1.8172 | 10.0000 | AID53346 |
[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) |
---|---|---|---|---|---|---|---|
[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) |
---|---|---|---|---|---|---|---|
Cyclin-dependent kinase 4 | Homo sapiens (human) | INH | 11.4000 | 6.7000 | 6.7000 | 6.7000 | AID738799 |
Cyclin-dependent kinase 6 | Homo sapiens (human) | INH | 11.4000 | 6.7000 | 6.7000 | 6.7000 | AID738799 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Synthesis and in vitro biological evaluation of 2,6,9-trisubstituted purines targeting multiple cyclin-dependent kinases. |
AID1356875 | Protection against cisplatin-induced cell death in neonatal mouse HEI-OC1 cells assessed as reduction in caspase-3/7 activity | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Second-Generation CDK2 Inhibitors for the Prevention of Cisplatin-Induced Hearing Loss. |
AID45825 | In vitro cytotoxic effect on CEM cancer cell line | 2002 | Bioorganic & medicinal chemistry letters, Nov-18, Volume: 12, Issue:22 | Synthesis and biological activity of olomoucine II. |
AID738803 | Cytotoxicity against human HOS cells assessed as reduction in number of viable cells after 72 hrs by fluorescence assay | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Synthesis and in vitro biological evaluation of 2,6,9-trisubstituted purines targeting multiple cyclin-dependent kinases. |
AID738799 | Inhibition of CDK (unknown origin) expressed in human ARN8 cells assessed as increase in p53-dependent transcriptional activity after 24 hrs by beta-galactosidase reporter gene assay | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Synthesis and in vitro biological evaluation of 2,6,9-trisubstituted purines targeting multiple cyclin-dependent kinases. |
AID477845 | Cytotoxicity against human MCF7 cells assessed as viable cells after 72 hrs by calcein AM assay | 2010 | Journal of natural products, Apr-23, Volume: 73, Issue:4 | Cytotoxic activities of several geranyl-substituted flavanones. |
AID738808 | Cytotoxicity against human K562 cells assessed as reduction in number of viable cells after 72 hrs by fluorescence assay | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Synthesis and in vitro biological evaluation of 2,6,9-trisubstituted purines targeting multiple cyclin-dependent kinases. |
AID738802 | Inhibition of CDK5/P35 (unknown origin) using histone H1 as substrate | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Synthesis and in vitro biological evaluation of 2,6,9-trisubstituted purines targeting multiple cyclin-dependent kinases. |
AID1204244 | Inhibition of Leishmania CRK3/CYC6 using histone H1/[gamma33-P]ATP as substrate at 30 uM after 30 mins relative to control | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | 2,6,9-Trisubstituted purines as CRK3 kinase inhibitors with antileishmanial activity in vitro. |
AID1204245 | Inhibition of Leishmania CRK3/CYC6 using histone H1/[gamma33-P]ATP as substrate after 30 mins | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | 2,6,9-Trisubstituted purines as CRK3 kinase inhibitors with antileishmanial activity in vitro. |
AID477847 | Cytotoxicity against human RPMI8226 cells assessed as viable cells after 72 hrs by calcein AM assay | 2010 | Journal of natural products, Apr-23, Volume: 73, Issue:4 | Cytotoxic activities of several geranyl-substituted flavanones. |
AID1356876 | Protection against cisplatin-induced toxicity in P3 mouse cochlear explants assessed as increase in outer hair cell count incubated for 24 hrs by phalloidin staining based confocal microscopy | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Second-Generation CDK2 Inhibitors for the Prevention of Cisplatin-Induced Hearing Loss. |
AID738800 | Inhibition of CDK9/CyclinT1 (unknown origin) using (YSPTSPS)2KK as substrate | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Synthesis and in vitro biological evaluation of 2,6,9-trisubstituted purines targeting multiple cyclin-dependent kinases. |
AID738807 | Cytotoxicity against human MCF7 cells assessed as reduction in number of viable cells after 72 hrs by fluorescence assay | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Synthesis and in vitro biological evaluation of 2,6,9-trisubstituted purines targeting multiple cyclin-dependent kinases. |
AID84363 | In vitro cytotoxic effect on HOS cancer cell line | 2002 | Bioorganic & medicinal chemistry letters, Nov-18, Volume: 12, Issue:22 | Synthesis and biological activity of olomoucine II. |
AID712278 | Agonist activity at N-type Cav2.2 channel expressed in tsA201 cell assessed as calcium current by whole-cell patch clamp method | 2012 | ACS medicinal chemistry letters, Dec-13, Volume: 3, Issue:12 | Synthesis and biological evaluation of a selective N- and p/q-type calcium channel agonist. |
AID477846 | Cytotoxicity against human CEM cells assessed as viable cells after 72 hrs by calcein AM assay | 2010 | Journal of natural products, Apr-23, Volume: 73, Issue:4 | Cytotoxic activities of several geranyl-substituted flavanones. |
AID53346 | Inhibition of recombinant Cyclin-dependent kinase 1-cyclin B | 2002 | Bioorganic & medicinal chemistry letters, Nov-18, Volume: 12, Issue:22 | Synthesis and biological activity of olomoucine II. |
AID1204242 | Cytotoxicity against human BJ cells assessed as cell viability at 30 uM after 72 hrs by fluorescence assay relative to control | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | 2,6,9-Trisubstituted purines as CRK3 kinase inhibitors with antileishmanial activity in vitro. |
AID738809 | Inhibition of CDK2/Cyclin E (unknown origin) expressed in Sf9 cells using histone H1 as substrate | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Synthesis and in vitro biological evaluation of 2,6,9-trisubstituted purines targeting multiple cyclin-dependent kinases. |
AID72433 | In vitro cytotoxic effect on G361 cancer cell line | 2002 | Bioorganic & medicinal chemistry letters, Nov-18, Volume: 12, Issue:22 | Synthesis and biological activity of olomoucine II. |
AID477848 | Cytotoxicity against human U266 cells assessed as viable cells after 72 hrs by calcein AM assay | 2010 | Journal of natural products, Apr-23, Volume: 73, Issue:4 | Cytotoxic activities of several geranyl-substituted flavanones. |
AID738804 | Cytotoxicity against human CEM cells assessed as reduction in number of viable cells after 72 hrs by fluorescence assay | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Synthesis and in vitro biological evaluation of 2,6,9-trisubstituted purines targeting multiple cyclin-dependent kinases. |
AID477850 | Cytotoxicity against human BJ cells assessed as viable cells after 72 hrs by calcein AM assay | 2010 | Journal of natural products, Apr-23, Volume: 73, Issue:4 | Cytotoxic activities of several geranyl-substituted flavanones. |
AID738806 | Cytotoxicity against human HCT116 cells assessed as reduction in number of viable cells after 72 hrs by fluorescence assay | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Synthesis and in vitro biological evaluation of 2,6,9-trisubstituted purines targeting multiple cyclin-dependent kinases. |
AID1204243 | Leshmanicidal activity against promastigote stage of Leishmania turanica MRHO/MN/08/BZ18 at 30 uM after 72 hrs by alamar blue staining-based fluorescence assay relative to control | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | 2,6,9-Trisubstituted purines as CRK3 kinase inhibitors with antileishmanial activity in vitro. |
AID1204246 | Leshmanicidal activity against promastigote stage of Leishmania turanica MRHO/MN/08/BZ18 after 72 hrs by alamar blue staining-based fluorescence assay | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | 2,6,9-Trisubstituted purines as CRK3 kinase inhibitors with antileishmanial activity in vitro. |
AID477849 | Cytotoxicity against human HeLa cells assessed as viable cells after 72 hrs by calcein AM assay | 2010 | Journal of natural products, Apr-23, Volume: 73, Issue:4 | Cytotoxic activities of several geranyl-substituted flavanones. |
AID1204247 | Leshmanicidal activity against promastigote stage of Leishmania major MHOM/IL/2003/LRC-L1025 at 30 uM after 72 hrs by alamar blue staining-based fluorescence assay | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | 2,6,9-Trisubstituted purines as CRK3 kinase inhibitors with antileishmanial activity in vitro. |
AID103422 | In vitro cytotoxic effect on MCF-7 cancer cell line | 2002 | Bioorganic & medicinal chemistry letters, Nov-18, Volume: 12, Issue:22 | Synthesis and biological activity of olomoucine II. |
AID738805 | Cytotoxicity against human G361 cells assessed as reduction in number of viable cells after 72 hrs by fluorescence assay | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Synthesis and in vitro biological evaluation of 2,6,9-trisubstituted purines targeting multiple cyclin-dependent kinases. |
AID94472 | In vitro cytotoxic effect on K562 cancer cell line | 2002 | Bioorganic & medicinal chemistry letters, Nov-18, Volume: 12, Issue:22 | Synthesis and biological activity of olomoucine II. |
AID1204248 | Leshmanicidal activity against promastigote stage of Leishmania donovani MHOM/SD/1962/1S-c12d at 30 uM after 72 hrs by alamar blue staining-based fluorescence assay | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | 2,6,9-Trisubstituted purines as CRK3 kinase inhibitors with antileishmanial activity in vitro. |
[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 | 4 (23.53) | 29.6817 |
2010's | 13 (76.47) | 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 (16.90) 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 | 17 (100.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |