Page last updated: 2024-12-10
sb 328437
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Description
SB 328437: a CC chemokine receptor-3 antagonist that inhibits binding of eotaxin and monocyte chemotactic protein-4 to eosinophils; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 10474776 |
| CHEMBL ID | 33227 |
| SCHEMBL ID | 3930225 |
| MeSH ID | M0375496 |
Synonyms (25)
| Synonym |
|---|
| sb 328437 |
| sb-328437 |
| CHEMBL33227 , |
| (s)-2-[(naphthalene-1-carbonyl)-amino]-3-(4-nitro-phenyl)-propionic acid methyl ester |
| bdbm50100021 |
| methyl (2s)-2-(naphthalene-2-carbonylamino)-3-(4-nitrophenyl)propanoate |
| n-(1-naphthalenylcarbonyl)-4-nitro-l-phenylalanine methyl ester |
| 247580-43-4 |
| l-phenylalanine, n-(1-naphthalenylcarbonyl)-4-nitro-, methyl ester |
| SCHEMBL3930225 |
| AKOS024457730 |
| DTXSID30440571 |
| sb 328437, >=98% (hplc) |
| J-015659 |
| NCGC00370865-01 |
| methyl (s)-2-(1-naphthamido)-3-(4-nitrophenyl)propanoate |
| methyl (2s)-2-(naphthalene-1-carbonylamino)-3-(4-nitrophenyl)propanoate |
| HMS3678E05 |
| HMS3414E05 |
| F81757 |
| MS-26166 |
| XJA58043 |
| CS-0027749 |
| HY-103363 |
| AKOS040745353 |
Research Excerpts
Bioavailability
| 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 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (9)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 3.0112 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 3.7908 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 2.1317 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| Interferon beta | Homo sapiens (human) | Potency | 3.7908 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 3.7908 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 3.7908 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 3.7908 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 1B | Homo sapiens (human) | IC50 (µMol) | 0.0070 | 0.0005 | 0.3975 | 6.5000 | AID44783 |
| C-C chemokine receptor type 3 | Homo sapiens (human) | IC50 (µMol) | 0.0506 | 0.0006 | 0.6041 | 9.0000 | AID42347; AID44779; AID44780; AID44781; AID44782; AID44783; AID44784; AID44785 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Activation Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| C-C chemokine receptor type 3 | Homo sapiens (human) | EC50 (µMol) | 0.7800 | 0.7800 | 0.7800 | 0.7800 | AID1327073 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (81)
Molecular Functions (25)
Ceullar Components (27)
Bioassays (15)
| 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. |
| 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. |
| 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. |
| 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. |
| AID42347 | Inhibitory activity against human eosinophil C-C chemokine receptor type 3 using [125I]- human eotaxin as the radioligand | 2001 | Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11 | Discovery of potent and selective phenylalanine derived CCR3 antagonists. Part 1. |
| AID44781 | Agonistic activity against C-C chemokine receptor type 3 by displacing Eotaxin-2 radioligand, using [Ca2+] mobilization assay | 2001 | Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11 | Discovery of potent and selective phenylalanine derived CCR3 antagonists. Part 1. |
| AID44780 | Agonistic activity against C-C chemokine receptor type 3 by displacing Eotaxin radioligand, using Eosinophil chemotaxis assay | 2001 | Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11 | Discovery of potent and selective phenylalanine derived CCR3 antagonists. Part 1. |
| AID44783 | Agonistic activity against C-C chemokine receptor type 3 by displacing [125I]-MCP-4 radioligand, using CCR3 binding assay | 2001 | Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11 | Discovery of potent and selective phenylalanine derived CCR3 antagonists. Part 1. |
| AID44782 | Agonistic activity against C-C chemokine receptor type 3 by displacing MCP-4 radioligand, using Eosinophil chemotaxis assay | 2001 | Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11 | Discovery of potent and selective phenylalanine derived CCR3 antagonists. Part 1. |
| AID44784 | Antagonist activity against C-C chemokine receptor type 3 | 2001 | Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11 | Discovery of potent and selective phenylalanine derived CCR3 receptor antagonists. Part 2. |
| AID1327073 | Antagonist activity at human EGFP-fused CCR3 expressed in mouse L1.2 cells assessed as inhibition of CCL11-induced chemotaxis measured after 1.5 hrs by PicoGreen dsDNA reagent-based assay | 2016 | Journal of natural products, 08-26, Volume: 79, Issue:8 | Neolignans from the Arils of Myristica fragrans as Potent Antagonists of CC Chemokine Receptor 3. |
| AID44785 | Binding affinity was determined towards C-C chemokine receptor type 3 using [125I]-labeled eotaxin as radioligand | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20 | Design and synthesis of novel CCR3 antagonists. |
| AID91101 | Ability to block the eotaxin induced intracellular calcium mobilization in primary human eosinophils was determined | 2001 | Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11 | Discovery of potent and selective phenylalanine derived CCR3 receptor antagonists. Part 2. |
| AID44779 | Agonistic activity against C-C chemokine receptor type 3 by displacing Eotaxin radioligand, using [Ca2+] mobilization assay | 2001 | Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11 | Discovery of potent and selective phenylalanine derived CCR3 antagonists. Part 1. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (15)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 5 (33.33) | 29.6817 |
| 2010's | 8 (53.33) | 24.3611 |
| 2020's | 2 (13.33) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Study Types
| 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% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||