NPS-1034: a protein kinase inhibitor that acts on MET and AXL; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 46194178 |
| CHEMBL ID | 3810063 |
| SCHEMBL ID | 1963111 |
| MeSH ID | M000594535 |
| Synonym |
|---|
| chembl3810063 , |
| bdbm50172077 |
| S7669 |
| SCHEMBL1963111 |
| AC-31427 |
| 1221713-92-3 |
| nps-1034 |
| n-(3-fluoro-4-((3-phenyl-1h-pyrrolo[2,3-b]pyridin-4-yl)oxy)phenyl)-2-(4-fluorophenyl)-1,5-dimethyl-3-oxo-2,3-dihydro-1h-pyrazole-4-carboxamide |
| AKOS032945148 |
| BCP15998 |
| nps1034;nps 1034 |
| BS-14709 |
| CS-0019643 |
| HY-100509 |
| nps1034 |
| nps 1034 |
| CCG-270007 |
| s4k , |
| NCGC00481564-01 |
| C71836 |
| 1-(4-fluorophenyl)-n-[3-fluoro-4-[(3-phenyl-1h-pyrrolo[2,3-b]pyridin-4-yl)oxy]phenyl]-2,3-dimethyl-5-oxopyrazole-4-carboxamide |
| WYB71392 |
| n-[3-fluoro-4-({3-phenyl-1h-pyrrolo[2,3-b]pyridin-4-yl}oxy)phenyl]-2-(4-fluorophenyl)-1,5-dimethyl-3-oxo-2,3-dihydro-1h-pyrazole-4-carboxamide |
| Z2573745727 |
| 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 (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| PPM1D protein | Homo sapiens (human) | Potency | 1.0435 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
| Interferon beta | Homo sapiens (human) | Potency | 1.0435 | 0.0033 | 9.1582 | 39.8107 | AID1347411 |
| [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) |
|---|---|---|---|---|---|---|---|
| Hepatocyte growth factor receptor | Homo sapiens (human) | IC50 (µMol) | 0.0480 | 0.0004 | 0.3722 | 10.0000 | AID1301427; AID1626949 |
| Tyrosine-protein kinase receptor UFO | Homo sapiens (human) | IC50 (µMol) | 0.1309 | 0.0007 | 0.4116 | 9.1000 | AID1301409; AID1301410; AID1626948; AID1733269 |
| Receptor-type tyrosine-protein kinase FLT3 | Homo sapiens (human) | IC50 (µMol) | 0.0631 | 0.0001 | 0.3275 | 9.5480 | AID1733272 |
| Tyrosine-protein kinase receptor TYRO3 | Homo sapiens (human) | IC50 (µMol) | 0.0100 | 0.0014 | 0.0573 | 0.3010 | AID1733271 |
| Tyrosine-protein kinase Mer | Homo sapiens (human) | IC50 (µMol) | 0.0016 | 0.0005 | 0.2863 | 4.9000 | AID1733270 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1733270 | Inhibition of 6His/thrombin cleavage site-fused Avi-tagged dephosphorylated MER (unknown origin) (R528 to M999 residues) using Axltide (CKKSRGDYMTMQJG-acid) peptide as substrate preincubated for 30 mins followed by substrate and ATP addition at Km concent | 2021 | Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6 | Generating Selective Leads for Mer Kinase Inhibitors-Example of a Comprehensive Lead-Generation Strategy. |
| AID1733273 | Intrinsic clearance in rat hepatocytes assessed per 10^6 cells | 2021 | Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6 | Generating Selective Leads for Mer Kinase Inhibitors-Example of a Comprehensive Lead-Generation Strategy. |
| AID1733272 | Inhibition of His6/TEV fused-GST-tagged Flt3 (unknown origin) (H564 to S993 residues) using Axltide (CKKSRGDYMTMQJ-acid) peptide as substrate preincubated for 30 mins followed by substrate and ATP addition at Km concentration measured after 75 mins by Rap | 2021 | Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6 | Generating Selective Leads for Mer Kinase Inhibitors-Example of a Comprehensive Lead-Generation Strategy. |
| AID1626948 | Inhibition of Axl (unknown origin) | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14 | 4-Oxo-1,4-dihydroquinoline-3-carboxamide Derivatives as New Axl Kinase Inhibitors. |
| AID1301410 | Inhibition of AXL (unknown origin) by cell based assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective. |
| AID1301427 | Inhibition of human recombinant MET expressed in Escherichia coli BL21 infected with T7 phage by qPCR method | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective. |
| AID1733274 | Intrinsic clearance in human liver microsomes | 2021 | Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6 | Generating Selective Leads for Mer Kinase Inhibitors-Example of a Comprehensive Lead-Generation Strategy. |
| AID1733271 | Inhibition of GST-tagged Tyro3 (unknown origin) (453 to 890 residues) using Axltide (KKSRGDYMTMQIG-acid) peptide as substrate preincubated for 30 mins followed by substrate and ATP addition at Km concentration measured after 180 mins by RapidFire LC-MS an | 2021 | Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6 | Generating Selective Leads for Mer Kinase Inhibitors-Example of a Comprehensive Lead-Generation Strategy. |
| AID1733269 | Inhibition of GST-tagged AXL (unknown origin) (464 to 485 residues) using Axltide (CKKSRGDYMTMQJG-acid) peptide as substrate preincubated for 30 mins followed by substrate and ATP addition at Km concentration measured after 180 mins by RapidFire LC-MS ana | 2021 | Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6 | Generating Selective Leads for Mer Kinase Inhibitors-Example of a Comprehensive Lead-Generation Strategy. |
| AID1301409 | Inhibition of human recombinant AXL expressed in Escherichia coli BL21 infected with T7 phage by qPCR method | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective. |
| AID1733275 | Distribution coefficient, logD of compound at pH 7.4 | 2021 | Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6 | Generating Selective Leads for Mer Kinase Inhibitors-Example of a Comprehensive Lead-Generation Strategy. |
| AID1626949 | Inhibition of Met (unknown origin) | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14 | 4-Oxo-1,4-dihydroquinoline-3-carboxamide Derivatives as New Axl Kinase Inhibitors. |
| AID1733276 | Aqueous solubility of the compound | 2021 | Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6 | Generating Selective Leads for Mer Kinase Inhibitors-Example of a Comprehensive Lead-Generation Strategy. |
| AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347414 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| 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. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| 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. |
| [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 | 6 (66.67) | 24.3611 |
| 2020's | 3 (33.33) | 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 (17.48) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (11.11%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 8 (88.89%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||