ID Source | ID |
---|---|
PubMed CID | 70679308 |
CHEMBL ID | 5178368 |
MeSH ID | M0573733 |
Synonym |
---|
1333377-65-3 |
HY-15217 |
chr-6494 |
CS-0994 |
3-(1h-indazol-5-yl)-n-propylimidazo[1,2-b]pyridazin-6-amine |
AKOS025149446 |
DTXSID90742629 |
CHEMBL5178368 , |
NCGC00370724-05 |
FT-0734501 |
chr6494 |
BCP06799 |
3-(1h-indazol-5-yl)-n-propylimidazo-[1,2-b]pyridazin-6-amine |
A899134 |
F84874 |
NCGC00370724-06 |
bdbm50587785 |
imidazo[1,2-b]pyridazin-6-amine, 3-(1h-indazol-5-yl)-n-propyl- |
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) |
---|---|---|---|---|---|---|---|
Tyrosine-protein kinase ABL1 | Homo sapiens (human) | IC50 (µMol) | 0.1620 | 0.0001 | 0.7128 | 10.0000 | AID1909342 |
Serine/threonine-protein kinase pim-1 | Homo sapiens (human) | IC50 (µMol) | 0.0290 | 0.0004 | 0.8871 | 10.0000 | AID1909326 |
Dual specificity protein kinase CLK1 | Mus musculus (house mouse) | IC50 (µMol) | 0.0080 | 0.0080 | 0.5127 | 4.3000 | AID1909330 |
Casein kinase I isoform epsilon | Homo sapiens (human) | IC50 (µMol) | 0.0990 | 0.0040 | 1.1150 | 9.5000 | AID1909338 |
Glycogen synthase kinase-3 beta | Homo sapiens (human) | IC50 (µMol) | 0.0530 | 0.0006 | 0.8013 | 10.0000 | AID1909336 |
Tyrosine-protein kinase JAK3 | Homo sapiens (human) | IC50 (µMol) | 0.1190 | 0.0001 | 0.4193 | 7.9200 | AID1909344 |
Cyclin-dependent-like kinase 5 | Homo sapiens (human) | IC50 (µMol) | 0.0410 | 0.0002 | 1.1832 | 10.0000 | AID1909339 |
Cyclin-dependent kinase 5 activator 1 | Homo sapiens (human) | IC50 (µMol) | 0.0410 | 0.0010 | 1.2898 | 10.0000 | AID1909339 |
Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0130 | 0.0100 | 0.5741 | 2.8000 | AID1909332 |
Serine/threonine-protein kinase haspin | Homo sapiens (human) | IC50 (µMol) | 0.0025 | 0.0020 | 0.1907 | 0.7700 | AID1846317; AID1909328 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1909337 | Inhibition of human recombinant CK1 epsilon expressed in baculovirus in sf9 insect cells assessed as residual activity at 1 uM using RRKHAAIGSpAYSITA as substrate measured after 30 mins in presence of ATP by ADP-Glo assay relative to control | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity. |
AID1909345 | Selectivity index, ratio of IC50 for recombinant mouse CLK1 expressed in bacteria to IC50 for recombinant human Haspin (470 to 798 residues) expressed in bacterial expression system | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity. |
AID1909336 | Inhibition of human recombinant GSK3beta expressed in baculovirus in Sf9 insect cells using YRRAAVPPSPSLSRHSSPHQSpEDEEE as substrate measured after 30 mins by ADP-Glo kinase assay | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity. |
AID1909325 | Inhibition of human recombinant CDK5/p25 expressed in bacterial expression system assessed as residual activity at 1 uM using histone H1 as substrate measured after 30 mins in presence of ATP by ADP-Glo assay relative to control | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity. |
AID1909342 | Inhibition of human recombinant ABL1 expressed in baculovirus sf9 insect cells using EAIYAAPFAKKK as substrate measured after 30 mins in presence of ATP by ADP-Glo assay | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity. |
AID1909334 | Inhibition of human recombinant CDK9 expressed in baculovirus insect Sf9 cells using YSPTSPSYSPTSPSYSPTSPSKKKK as substrate measured after 30 mins in presence of ATP by ADP-Glo assay | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity. |
AID1909330 | Inhibition of recombinant mouse CLK1 expressed in bacteria using GRSRSRSRSRSR as substrate in presence of ATP measured after 30 mins by ADP-Glo assay | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity. |
AID1909359 | Inhibition of human haspin activity in HCT-116 assessed as induction of phosphorylation of H3 on threonine 3 at 1 uM incubated for 16 hrs by Immunofluorescent assay | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity. |
AID1909331 | Inhibition of recombinant rat DYRK1A (1 to 499 residues) expressed in bacterial expression system assessed as residual activity at 1 uM using KKISGRLSPIMTEQ as substrate measured after 30 mins in presence of ATP by ADP-Glo assay relative to control | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity. |
AID1909339 | Inhibition of human recombinant CDK5/p25 expressed in bacterial expression system using histone H1 as substrate in presence of ATP at measured after 30 mins by ADP-Glo assay | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity. |
AID1909340 | Inhibition of recombinant human PIM1 expressed in bacterial expression system assessed as residual activity at 1 uM using histone H1 as substrate measured after 30 mins in presence of ATP by ADP-Glo assay relative to control | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity. |
AID1909335 | Inhibition of human recombinant GSK3beta expressed in baculovirus in Sf9 insect cells assessed as residual activity at 1 uM using YRRAAVPPSPSLSRHSSPHQSpEDEEE as substrate measured after 30 mins in presence of ATP by ADP-Glo kinase assay relative to contro | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity. |
AID1909327 | Inhibition of recombinant human Haspin (470 to 798 residues) expressed in bacterial expression system assessed as residual activity at 1 uM using ARTKQTARKSTGGKAPRKQLA as substrate measured after 30 mins in presence of ATP by ADP-Glo assay relative to con | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity. |
AID1909343 | Inhibition of human recombinant JAK3 expressed in baculovirus sf9 insect cells assessed as residual activity at 1 uM using GGEEEEYFELVKKKK as substrate measured after 30 mins in presence of ATP by ADP-Glo assay relative to control | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity. |
AID1909341 | Inhibition of human recombinant ABL1 expressed in baculovirus sf9 insect cells assessed as residual activity at 1 uM using EAIYAAPFAKKK as substrate measured after 30 mins in presence of ATP by ADP-Glo assay relative to control | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity. |
AID1846317 | Inhibition of haspin (unknown origin) by FRET assay | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Recent advances in development of hetero-bivalent kinase inhibitors. |
AID1909329 | Inhibition of recombinant mouse CLK1 expressed in bacteria assessed as residual activity at 1 uM using GRSRSRSRSRSR as substrate measured after 30 mins in presence of ATP by ADP-Glo assay relative to control | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity. |
AID1909326 | Inhibition of recombinant human PIM1 expressed in bacterial expression system using histone H1 as substrate measured after 30 mins in presence of ATP by ADP-Glo assay | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity. |
AID1909332 | Inhibition of recombinant rat DYRK1A (1 to 499 residues ) expressed in bacterial expression system using KKISGRLSPIMTEQ as substrate measured after 30 mins in presence of ATP by ADP-Glo assay | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity. |
AID1909328 | Inhibition of recombinant human Haspin (470 to 798 residues) expressed in bacterial expression system using ARTKQTARKSTGGKAPRKQLA as substrate measured after 30 mins in presence of ATP by ADP-Glo assay | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity. |
AID1909344 | Inhibition of human recombinant JAK3 expressed in baculovirus sf9 insect cells using GGEEEEYFELVKKKK as substrate measured after 30 mins in presence of ATP by ADP-Glo assay | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity. |
AID1909338 | Inhibition of human recombinant CK1 epsilon expressed in baculovirus in sf9 insect cells using RRKHAAIGSpAYSITA as substrate in presence of ATP measured after 30 mins by ADP-Glo assay | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity. |
AID1909333 | Inhibition of human recombinant CDK9/CyclinT expressed in baculovirus insect Sf9 cells assessed as residual activity at 1 uM using YSPTSPSYSPTSPSYSPTSPSKKKK as substrate measured after 30 mins in presence of ATP by ADP-Glo assay relative to control | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity. |
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. |
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. |
[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 | 1 (20.00) | 24.3611 |
2020's | 4 (80.00) | 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 (18.01) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 0 (0.00%) | 5.53% |
Reviews | 1 (20.00%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 4 (80.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |