NBI-74330: CXC chemokine receptor 3 (CXCR3) antagonist; structure in first source [MeSH]
| ID Source | ID |
|---|---|
| PubMed CID | 10167713 |
| CHEMBL ID | 4173833 |
| SCHEMBL ID | 15064525 |
| MeSH ID | M0486859 |
| Synonym |
|---|
| LS-15325 |
| (plusmn)-nbi 74330 |
| n-[1-[3-(4-ethoxyphenyl)-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-2-[4-fluoro-3-(trifluoromethyl)phenyl]-n-(pyridin-3-ylmethyl)acetamide |
| nbi74330 |
| gtpl839 |
| nbi-74330 |
| 855527-92-3 |
| (+/-)-nbi 74330 |
| 473722-68-8 |
| n-1-[(3-4(-ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-4-fluoro-n-(3-pyridinylmethyl)-3-(trifluoromethyl)benzeneacetamide |
| SCHEMBL15064525 |
| AKOS024458204 |
| NCGC00379149-01 |
| ( inverted exclamation marka)-nbi 74330 |
| Q27087862 |
| xmrgquduvgrcbs-uhfffaoysa-n |
| BCP34091 |
| nbi 74330; nbi74330 |
| HMS3747I15 |
| n-{1-[3-(4-ethoxyphenyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin- 2-yl]ethyl}-2-[4-fluoro-3-(trifluoromethyl)phenyl]-n-(3-pyridinyl methyl)acetamide |
| A923478 |
| CHEMBL4173833 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
|---|---|---|---|---|
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 2.6837 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 4.7724 | AID1645842 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 23.9185 | AID1645840 |
| Interferon beta | Homo sapiens (human) | Potency | 4.7724 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 4.7724 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 4.7724 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 4.7724 | AID1645842 |
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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 ISSN: 1091-6490 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 ISSN: 2472-5560 | 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 ISSN: 1521-0111 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| 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 ISSN: 1091-6490 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| 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 ISSN: 1521-0111 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1359948 | Negative allosteric modulation of PK1-tagged CXCR3 (unknown origin) expressed in HEK293T cells co-expressing beta-arrestin/beta-Gal enzyme chimera assessed as inhibition of CXCL11-induced beta-arrestin recruitment at 10 uM after 4 hrs by chemiluminescence | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154ISSN: 1768-3254 | Insight into structural requirements for selective and/or dual CXCR3 and CXCR4 allosteric modulators. |
| AID1346862 | Human CXCR3 (Chemokine receptors) | 2005 | The Journal of pharmacology and experimental therapeutics, Jun, Volume: 313, Issue:3 ISSN: 0022-3565 | Pharmacological characterization of CXC chemokine receptor 3 ligands and a small molecule antagonist. |
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 4 (26.67) | 29.6817 |
| 2010's | 7 (46.67) | 24.3611 |
| 2020's | 4 (26.67) | 2.80 |
| 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 | 15 (100.00%) | 84.16% |
| Substance | Studies | Classes | Roles | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| niacinamide | pyridine alkaloid; pyridinecarboxamide; vitamin B3 | anti-inflammatory agent; antioxidant; cofactor; EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor; EC 3.5.1.98 (histone deacetylase) inhibitor; Escherichia coli metabolite; geroprotector; human urinary metabolite; metabolite; mouse metabolite; neuroprotective agent; Saccharomyces cerevisiae metabolite; Sir2 inhibitor | 2014 | 2014 | 10.0 | high | 0 | 0 | 0 | 0 | 1 | 0 | |
| guanosine 5'-o-(3-thiotriphosphate) | nucleoside triphosphate analogue | 2005 | 2005 | 19.0 | high | 0 | 0 | 0 | 1 | 0 | 0 |
| Condition | Indicated | Studies | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Adjuvant Arthritis | 0 | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
| Alloxan Diabetes | 0 | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Arthritis, Rheumatoid | 0 | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
| Atherogenesis | 0 | 2008 | 2008 | 16.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Atherosclerosis | 0 | 2008 | 2008 | 16.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Autoimmune Diabetes | 0 | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Congenital Zika Syndrome | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Diabetes Mellitus, Type 1 | 0 | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Disease Models, Animal | 0 | 2008 | 2020 | 8.7 | medium | 0 | 0 | 0 | 1 | 2 | 0 | |
| Hepatitis C | 0 | 2009 | 2009 | 15.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Hepatitis, Viral, Non-A, Non-B, Parenterally-Transmitted | 0 | 2009 | 2009 | 15.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Inflammation | 0 | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
| Innate Inflammatory Response | 0 | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
| Lesion of Sciatic Nerve | 0 | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Nerve Pain | 0 | 2018 | 2021 | 4.5 | low | 0 | 0 | 0 | 0 | 1 | 1 | |
| Neuralgia | 0 | 2018 | 2021 | 4.5 | low | 0 | 0 | 0 | 0 | 1 | 1 | |
| Rheumatoid Arthritis | 0 | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
| Zika Virus Infection | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Article | Year |
|---|---|
| Analysis of the pharmacokinetic/pharmacodynamic relationship of a small molecule CXCR3 antagonist, NBI-74330, using a murine CXCR3 internalization assay. British journal of pharmacology, , Volume: 152, Issue:8 | 2007 |
| Article | Year |
|---|---|
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular pharmacology, , Volume: 96, Issue:5 | 2019 |
| Article | Year |
|---|---|
| Analysis of the pharmacokinetic/pharmacodynamic relationship of a small molecule CXCR3 antagonist, NBI-74330, using a murine CXCR3 internalization assay. British journal of pharmacology, , Volume: 152, Issue:8 | 2007 |