Page last updated: 2024-12-11
cp 135807
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
CP 135807: a 5-HT(1D) agonist; RN given for (R)-isomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 5487088 |
| CHEMBL ID | 83597 |
| SCHEMBL ID | 7851221 |
| MeSH ID | M0267225 |
Synonyms (34)
| Synonym |
|---|
| CHEMBL83597 , |
| cp-135807 |
| [3-((r)-1-methyl-pyrrolidin-2-ylmethyl)-1h-indol-5-yl]-(3-nitro-pyridin-2-yl)-amine |
| bdbm50039564 |
| (r)-3-((1-methyl-2-pyrrolidinyl)methyl)-n-(3-nitro-2-pyridinyl)-1h-indol-5-amine |
| 1h-indol-5-amine, 3-((1-methyl-2-pyrrolidinyl)methyl)-n-(3-nitro-2-pyridinyl)-, (r)- |
| cp 135807 |
| 3-(n-methylpyrrolidin-2-ylmethyl)-5-(3-nitropyrid-2-ylamino)-1h-indole |
| cp 135,807 |
| 3-[[(2r)-1-methylpyrrolidin-2-yl]methyl]-n-(3-nitropyridin-2-yl)-1h-indol-5-amine |
| HMS3263P18 |
| 151272-90-1 |
| unii-te348fq6da |
| te348fq6da , |
| 3-[[(2r)-1-methyl-2-pyrrolidinyl]methyl]-n-(3-nitro-2-pyridinyl)-1h-indol-5-amine |
| CCG-222582 |
| YPFIYPNOWVPAPR-OAHLLOKOSA-N , |
| (r)-3-(n-methylpyrrolidin-2-ylmethyl)-5-(3-nitropyrid-2-ylamino)-1h-indole |
| NCGC00261963-01 |
| tox21_501278 |
| AKOS024457797 |
| SCHEMBL7851221 |
| (r)-3-((1-methylpyrrolidin-2-yl)methyl)-n-(3-nitropyridin-2-yl)-1h-indol-5-amine |
| DTXSID10164748 |
| (r)-3-[1-methylpyrrolidin-2-ylmethyl]-5-(3-nitropyridin-2-ylamino)-1h-indole |
| cp-135807, >=98% (hplc) |
| J-008798 |
| NCGC00370978-02 |
| 3-[[(2r)-1-methylpyrrolidin-2-yl]methyl]-n-(3-nitro-2-pyridyl)-1h-indol-5-amine |
| cp135807 |
| BGA27290 |
| 1h-indol-5-amine, 3-[[(2r)-1-methyl-2-pyrrolidinyl]methyl]-n-(3-nitro-2-pyridinyl)- |
| E98680 |
| AKOS040745155 |
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 (14)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Fumarate hydratase | Homo sapiens (human) | Potency | 4.4668 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 37.9083 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 18.9991 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 3.0112 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| polyprotein | Zika virus | Potency | 4.4668 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
| Interferon beta | Homo sapiens (human) | Potency | 18.9991 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 18.9991 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 18.9991 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 18.9991 | 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) |
|---|---|---|---|---|---|---|---|
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0330 | 0.0002 | 1.8742 | 10.0000 | AID3731 |
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0330 | 0.0003 | 1.3833 | 8.4000 | AID3731 |
| Alpha-1D adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0330 | 0.0002 | 1.2704 | 10.0000 | AID3731 |
| 5-hydroxytryptamine receptor 1D | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0031 | 0.0031 | 1.7360 | 7.8000 | AID4873 |
| Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0330 | 0.0000 | 1.8194 | 10.0000 | AID3731 |
| [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) |
|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.0470 | 0.0054 | 3.2510 | 20.9400 | AID3709 |
| 5-hydroxytryptamine receptor 1D | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.0013 | 0.0013 | 0.0388 | 0.0970 | AID4872 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (45)
Molecular Functions (18)
Ceullar Components (22)
Bioassays (17)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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. |
| 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. |
| 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. |
| AID1347059 | CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID1347058 | CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID1347057 | CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID1347410 | qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library | 2019 | Cellular signalling, 08, Volume: 60 | A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening. |
| AID1347405 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection | 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. |
| AID1347151 | Optimization of GU AMC 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. |
| AID235510 | Selectivity value is the ratio between EC50 values of 5-HT1A and 5-HT1D receptors | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16 | 5-[(3-nitropyrid-2-yl)amino]indoles: novel serotonin agonists with selectivity for the 5-HT1D receptor. Variation of the C3 substituent on the indole template leads to increased 5-HT1D receptor selectivity. |
| AID4873 | Binding affinity was measured against serotonin 5-hydroxytryptamine 1D receptor | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16 | 5-[(3-nitropyrid-2-yl)amino]indoles: novel serotonin agonists with selectivity for the 5-HT1D receptor. Variation of the C3 substituent on the indole template leads to increased 5-HT1D receptor selectivity. |
| AID4872 | Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1D receptor | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16 | 5-[(3-nitropyrid-2-yl)amino]indoles: novel serotonin agonists with selectivity for the 5-HT1D receptor. Variation of the C3 substituent on the indole template leads to increased 5-HT1D receptor selectivity. |
| AID3709 | Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16 | 5-[(3-nitropyrid-2-yl)amino]indoles: novel serotonin agonists with selectivity for the 5-HT1D receptor. Variation of the C3 substituent on the indole template leads to increased 5-HT1D receptor selectivity. |
| AID3731 | Binding affinity was measured against serotonin 5-hydroxytryptamine 1A receptor | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16 | 5-[(3-nitropyrid-2-yl)amino]indoles: novel serotonin agonists with selectivity for the 5-HT1D receptor. Variation of the C3 substituent on the indole template leads to increased 5-HT1D receptor selectivity. |
| AID235511 | Selectivity value is the ratio between IC50 values of 5-HT1A and 5-HT1D receptors | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16 | 5-[(3-nitropyrid-2-yl)amino]indoles: novel serotonin agonists with selectivity for the 5-HT1D receptor. Variation of the C3 substituent on the indole template leads to increased 5-HT1D receptor selectivity. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (11)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 4 (36.36) | 18.2507 |
| 2000's | 1 (9.09) | 29.6817 |
| 2010's | 3 (27.27) | 24.3611 |
| 2020's | 3 (27.27) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 12.71
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 weak demand-to-supply ratio for research on this compound.
| This Compound (12.71) All Compounds (24.57) |
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 | 12 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||