Page last updated: 2024-12-10
cp 154526
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Description
CP 154526: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 5311055 |
| CHEMBL ID | 9946 |
| CHEMBL ID | 475903 |
| SCHEMBL ID | 5707848 |
| MeSH ID | M0266353 |
| PubMed CID | 11475094 |
| SCHEMBL ID | 7165019 |
| MeSH ID | M0266353 |
Synonyms (56)
| Synonym |
|---|
| cp-154526 |
| PDSP2_001283 |
| PDSP1_001299 , |
| cp154526 |
| CHEMBL9946 , |
| n-butyl-n-ethyl-2,5-dimethyl-7-(2,4,6-trimethylphenyl)pyrrolo[2,3-d]pyrimidin-4-amine |
| cp 154,526 |
| n-butyl-n-ethyl-7-mesityl-2,5-dimethyl-7h-pyrrolo[2,3-d]pyrimidin-4-amine |
| bdbm50058163 |
| cp-154526-1 |
| CHEMBL475903 , |
| butyl-(2,5-dimethyl-7-(2,4,6-trimethylphenyl)-7h-pyrrolo(2,3-d)pyrimidin-4-yl)ethylamine |
| cp-154,526 |
| n-butyl-n-ethyl-2,5-dimethyl-7-(2,4,6-trimethylphenyl)pyrrolo(2,3-d)pyrimidin-4-amine |
| 9a549fb00r , |
| 157286-86-7 |
| unii-9a549fb00r |
| bdbm50369802 |
| AB07693 |
| cp154,526 |
| gtpl3495 |
| n-butyl-n-ethyl-2,5-dimethyl-7-(2,4,6-trimethylphenyl)pyrrolo[3,2-e]pyrimidin-4-amine |
| SCHEMBL5707848 |
| FHQYJZCJRZHINA-UHFFFAOYSA-N |
| butyl-ethyl-[2,5-dimethyl-7-(2,4,6-trimethylphenyl)-7h-pyrrolo[2,3-d]pyrimidin-4-yl]amine |
| 7h-pyrrolo(2,3-d)pyrimidin-4-amine, n-butyl-n-ethyl-2,5-dimethyl-7-(2,4,6-trimethylphenyl)- |
| NCGC00378725-02 |
| n-butyl-n-ethyl-2,5-dimethyl-7-(2,4,6-trimethylphenyl)-7h-pyrrolo[2,3-d]pyrimidin-4-amine |
| AKOS032946677 |
| Q5013574 |
| BCP26372 |
| cp-154526;cp 154526;cp 154,526; cp-154,526; cp154,526 |
| DTXSID201027582 |
| 7h-pyrrolo[2,3-d]pyrimidin-4-amine, n-butyl-n-ethyl-2,5-dimethyl-7-(2,4,6-trimethylphenyl)- |
| FT-0665210 |
| cp 154526 |
| SCHEMBL7165019 |
| BCP9000548 |
| cp-154526 hydrochloride |
| 257639-98-8 |
| cp 154526 hydrochloride |
| n-butyl-n-ethyl-2,5-dimethyl-7-(2,4,6-trimethylphenyl)-7h-pyrrolo[2,3-d]pyrimidin-4-amine hydrochloride |
| CCG-221954 |
| NCGC00261335-01 |
| tox21_500650 |
| butyl-[2,5-dimethyl-7-(2,4,6-trimethyl-phenyl)-7h-pyrrolo[2,3-d]pyrimidin-4-yl]-ethyl-amine hydrochloride |
| AKOS024457291 |
| cp-154526 hydrochloride, >=98% (hplc) |
| J-009400 |
| J-016123 |
| DTXSID401018042 |
| n-butyl-n-ethyl-2,5-dimethyl-7-(2,4,6-trimethylphenyl)pyrrolo[2,3-d]pyrimidin-4-amine;hydrochloride |
| n-butyl-n-ethyl-7-mesityl-2,5-dimethyl-7h-pyrrolo[2,3-d]pyrimidin-4-amine hydrochloride |
| 7h-pyrrolo[2,3-d]pyrimidin-4-amine, n-butyl-n-ethyl-2,5-dimethyl-7-(2,4,6-trimethylphenyl)-, (hydrochloride) (1:1) |
| cp-154526hydrochloride |
| E98765 |
Research Excerpts
Pharmacokinetics
| Excerpt | Reference | Relevance |
|---|---|---|
| " On the basis of this property and lipophilicity differences, six of these compounds (4d,i,n,x, 8k, 9a) were initially chosen for rat pharmacokinetic (PK) studies." | ( Synthesis, corticotropin-releasing factor receptor binding affinity, and pharmacokinetic properties of triazolo-, imidazo-, and pyrrolopyrimidines and -pyridines. Aldrich, PE; Arvanitis, A; Bakthavatchalam, R; Beck, JP; Cheeseman, RS; Chidester, D; Chien, BM; Chorvat, RJ; Cocuzza, AJ; Curry, M; Fernandez, CH; Fitzgerald, LW; Gilligan, PJ; Hobbs, FW; Hodge, CN; Huang, SM; Klaczkiewicz, JD; Krenitsky, P; Rescinito, JP; Shen, HL; Wasserman, ZR; Wilde, RG; Wong, YN; Yarem, JA; Zaczek, R, 1999) | 0.3 |
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 |
| " Oral bioavailability reached 27%." | ( Brain pharmacokinetics of a nonpeptidic corticotropin-releasing factor receptor antagonist. Bruelisauer, A; Enz, A; Keller, C; Lemaire, M, 2002) | 0.31 |
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| " Drug intake was decreased across several doses of cocaine, with the dose-response curve for cocaine self-administration shifted downward and flattened, suggesting that CP-154,526 decreased cocaine reinforcement." | ( Effects of the CRH receptor antagonist CP-154,526 on intravenous cocaine self-administration in rats. Goeders, NE; Guerin, GF, 2000) | 0.31 |
| " In contrast to acute administration, a challenge injection of LY379268 after repeated dosing (10 mg/kg x days) did not alter basal NE." | ( Comparison of the effects of diazepam, the CRF1 antagonist CP-154,526 and the group II mGlu receptor agonist LY379268 on stress-evoked extracellular norepinephrine levels. Baccei, CS; Bristow, LJ; Correa, LD; Lorrain, DS, 2005) | 0.33 |
| " For these studies, animals were dosed with CP-154,526 (3, 10, 30 mg/kg) and NBI 27914 (1-30 mg/kg) 1 h prior to the assessment of tactile, thermal or mechanical hypersensitivity, respectively." | ( Pain is a salient "stressor" that is mediated by corticotropin-releasing factor-1 receptors. Cummons, T; Harrison, JE; Hummel, M; Kennedy, JD; Lu, P; Mark, L; Whiteside, GT, 2010) | 0.36 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (10)
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 | 6.0081 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 11.9877 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Interferon beta | Homo sapiens (human) | Potency | 11.9877 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 11.9877 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 11.9877 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 11.9877 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 13.5843 | 0.0015 | 30.6073 | 15,848.9004 | AID1224819; AID1224820; AID1224821; AID1224823 |
| [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) |
|---|---|---|---|---|---|---|---|
| Corticotropin-releasing factor receptor 1 | Homo sapiens (human) | IC50 (µMol) | 0.0134 | 0.0007 | 0.0649 | 0.3400 | AID308979; AID591214 |
| Corticotropin-releasing factor receptor 1 | Homo sapiens (human) | Ki | 0.0073 | 0.0008 | 0.0102 | 0.2400 | AID239655; AID314071; AID362068; AID53829; AID53831; AID53968; AID53972; AID53975; AID53978; AID54135; AID609182 |
| Corticotropin-releasing factor receptor 1 | Rattus norvegicus (Norway rat) | Ki | 0.0027 | 0.0010 | 0.0029 | 0.0050 | AID53978 |
| Corticotropin-releasing factor receptor 2 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 0.0010 | 0.0015 | 0.0020 | AID54136 |
| Corticotropin-releasing factor receptor 1 | Homo sapiens (human) | Ki | 0.0022 | 0.0008 | 0.0102 | 0.2400 | AID223385; AID53832 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (59)
Molecular Functions (22)
Ceullar Components (24)
Bioassays (51)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID308979 | Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane | 2007 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18 | Novel substituted tetrahydrotriazaacenaphthylene derivatives as potent CRF1 receptor antagonists. |
| AID53979 | Tested for in vivo activity and binding affinity to human Corticotropin releasing factor receptor 1; In activie | 2001 | Bioorganic & medicinal chemistry letters, Dec-17, Volume: 11, Issue:24 | 1-Alkyl-3-amino-5-aryl-1H-[1,2,4]triazoles: novel synthesis via cyclization of N-acyl-S-methylisothioureas with alkylhydrazines and their potent corticotropin-releasing factor-1 (CRF(1)) receptor antagonist activities. |
| AID15519 | Plasma clearance in rat | 1997 | Journal of medicinal chemistry, May-23, Volume: 40, Issue:11 | Synthesis and oral efficacy of a 4-(butylethylamino)pyrrolo[2,3-d]pyrimidine: a centrally active corticotropin-releasing factor1 receptor antagonist. |
| AID53831 | Antagonistic activity for Corticotropin releasing factor receptor 1 | 1999 | Bioorganic & medicinal chemistry letters, Apr-05, Volume: 9, Issue:7 | Use of the Suzuki reaction for the synthesis of aryl-substituted heterocycles as corticotropin-releasing hormone (CRH) antagonists. |
| AID609182 | Antagonist activity at human CRF-1 receptor | 2011 | Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12 | Discovery of N-(1-ethylpropyl)-[3-methoxy-5-(2-methoxy-4-trifluoromethoxyphenyl)-6-methyl-pyrazin-2-yl]amine 59 (NGD 98-2): an orally active corticotropin releasing factor-1 (CRF-1) receptor antagonist. |
| AID53978 | Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells | 2002 | Bioorganic & medicinal chemistry letters, Aug-19, Volume: 12, Issue:16 | 3-Aryl pyrazolo[4,3-d]pyrimidine derivatives: Nonpeptide CRF-1 antagonists. |
| AID237197 | Terminal half life in rat was determined upon oral administration | 2005 | Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16 | Design and synthesis of tricyclic imidazo[4,5-b]pyridin-2-ones as corticotropin-releasing factor-1 antagonists. |
| AID591214 | Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8 | Discovery of pyrrolo[2,3-d]pyrimidin-4-ones as corticotropin-releasing factor 1 receptor antagonists with a carbonyl-based hydrogen bonding acceptor. |
| AID239655 | Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells | 2005 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 15, Issue:17 | Synthesis, structure-activity relationships, and anxiolytic activity of 7-aryl-6,7-dihydroimidazoimidazole corticotropin-releasing factor 1 receptor antagonists. |
| AID53968 | Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells | 1999 | Journal of medicinal chemistry, Mar-11, Volume: 42, Issue:5 | Synthesis, corticotropin-releasing factor receptor binding affinity, and pharmacokinetic properties of triazolo-, imidazo-, and pyrrolopyrimidines and -pyridines. |
| AID25377 | Half life in rat | 1997 | Journal of medicinal chemistry, May-23, Volume: 40, Issue:11 | Synthesis and oral efficacy of a 4-(butylethylamino)pyrrolo[2,3-d]pyrimidine: a centrally active corticotropin-releasing factor1 receptor antagonist. |
| AID362068 | Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells | 2008 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 18, Issue:16 | 2-Arylpyrimidines: novel CRF-1 receptor antagonists. |
| AID236297 | Volume distribution in rat was determined upon peroral administration | 2005 | Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16 | Design and synthesis of tricyclic imidazo[4,5-b]pyridin-2-ones as corticotropin-releasing factor-1 antagonists. |
| AID54136 | Inhibition of binding of [125I]-Tyr0-sauvagine to Corticotropin releasing hormone receptor 2 (CRF2) | 1997 | Journal of medicinal chemistry, May-23, Volume: 40, Issue:11 | Synthesis and oral efficacy of a 4-(butylethylamino)pyrrolo[2,3-d]pyrimidine: a centrally active corticotropin-releasing factor1 receptor antagonist. |
| AID14001 | Oral bioavailability in rat | 1997 | Journal of medicinal chemistry, May-23, Volume: 40, Issue:11 | Synthesis and oral efficacy of a 4-(butylethylamino)pyrrolo[2,3-d]pyrimidine: a centrally active corticotropin-releasing factor1 receptor antagonist. |
| AID54134 | Inhibition of binding of 70 pM [125I]-Try0-o-Corticotropin-releasing Factor (CFR) to Corticotropin releasing hormone receptor 1 in Rat brain membrane | 1997 | Journal of medicinal chemistry, May-23, Volume: 40, Issue:11 | Synthesis and oral efficacy of a 4-(butylethylamino)pyrrolo[2,3-d]pyrimidine: a centrally active corticotropin-releasing factor1 receptor antagonist. |
| AID243181 | Displacement of [125I]o-CRF from recombinant human CRF receptors expressed in Chinese Hamster Ovary (CHO) cell membranes | 2005 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 15, Issue:16 | Substituted tetraazaacenaphthylenes as potent CRF1 receptor antagonists for the treatment of depression and anxiety. |
| AID53975 | Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells | 1998 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16 | Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists. |
| AID53829 | Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells | 1999 | Bioorganic & medicinal chemistry letters, Apr-05, Volume: 9, Issue:7 | 4-Aryl-2-anilinopyrimidines as corticotropin-releasing hormone (CRH) antagonists. |
| AID53972 | Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell. | 2003 | Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22 | 2-arylaminothiazoles as high-affinity corticotropin-releasing factor 1 receptor (CRF1R) antagonists: synthesis, binding studies and behavioral efficacy. |
| AID54135 | Binding affinity against [125I]-Try0-o-Corticotropin-releasing Factor to Corticotropin releasing hormone receptor 1 from ovine | 1997 | Journal of medicinal chemistry, May-23, Volume: 40, Issue:11 | Synthesis and oral efficacy of a 4-(butylethylamino)pyrrolo[2,3-d]pyrimidine: a centrally active corticotropin-releasing factor1 receptor antagonist. |
| AID22439 | Volume of distribution in steady state in rat | 1997 | Journal of medicinal chemistry, May-23, Volume: 40, Issue:11 | Synthesis and oral efficacy of a 4-(butylethylamino)pyrrolo[2,3-d]pyrimidine: a centrally active corticotropin-releasing factor1 receptor antagonist. |
| AID314071 | Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3 | The design, synthesis and structure-activity relationships of 1-aryl-4-aminoalkylisoquinolines: a novel series of CRF-1 receptor antagonists. |
| AID13866 | Maximal plasma concentration in rat | 1997 | Journal of medicinal chemistry, May-23, Volume: 40, Issue:11 | Synthesis and oral efficacy of a 4-(butylethylamino)pyrrolo[2,3-d]pyrimidine: a centrally active corticotropin-releasing factor1 receptor antagonist. |
| 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. |
| 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. |
| 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. |
| AID1345709 | Rat CRF1 receptor (Corticotropin-releasing factor receptors) | 1996 | European journal of pharmacology, Aug-08, Volume: 309, Issue:2 | A non peptidic corticotropin releasing factor receptor antagonist attenuates fever and exhibits anxiolytic-like activity. |
| 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. |
| AID1347167 | Vero cells viability 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. |
| AID1347169 | Tertiary RLuc qRT-PCR qHTS assay 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. |
| 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. |
| AID1347168 | HepG2 cells viability 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. |
| 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. |
| 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. |
| AID1347152 | Confirmatory screen NINDS AMC 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. |
| AID1347161 | Confirmatory 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. |
| AID1347153 | Confirmatory screen GU AMC 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. |
| 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. |
| AID1347149 | Furin counterscreen 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. |
| AID53832 | Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1 | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3 | 4-(1,3-Dimethoxyprop-2-ylamino)-2,7-dimethyl-8-(2, 4-dichlorophenyl)pyrazolo[1,5-a]-1,3,5-triazine: a potent, orally bioavailable CRF(1) receptor antagonist. |
| AID223385 | binding affinity for human CRF1 receptor in IMR32 neuroblastoma cells | 2000 | Journal of medicinal chemistry, May-04, Volume: 43, Issue:9 | Corticotropin releasing factor (CRF) receptor modulators: progress and opportunities for new therapeutic agents. |
| AID193158 | %binding inhibition in rat ex vivo assay after one hour | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3 | 4-(1,3-Dimethoxyprop-2-ylamino)-2,7-dimethyl-8-(2, 4-dichlorophenyl)pyrazolo[1,5-a]-1,3,5-triazine: a potent, orally bioavailable CRF(1) receptor antagonist. |
| AID179446 | 50% inhibitory concentration to antagonize ACTH secretion | 2000 | Journal of medicinal chemistry, May-04, Volume: 43, Issue:9 | Corticotropin releasing factor (CRF) receptor modulators: progress and opportunities for new therapeutic agents. |
| AID353807 | Aqueous solubility at pH 7 | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists. |
| AID353806 | Lipophilicity log P of the compound | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists. |
| AID173551 | Dose (ip) that completely reverses the r/h-CRF-enhanced acoustic startle of rats | 2000 | Journal of medicinal chemistry, May-04, Volume: 43, Issue:9 | Corticotropin releasing factor (CRF) receptor modulators: progress and opportunities for new therapeutic agents. |
| AID193159 | %binding inhibition in rat ex vivo assay after three hours | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3 | 4-(1,3-Dimethoxyprop-2-ylamino)-2,7-dimethyl-8-(2, 4-dichlorophenyl)pyrazolo[1,5-a]-1,3,5-triazine: a potent, orally bioavailable CRF(1) receptor antagonist. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (141)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 13 (9.22) | 18.2507 |
| 2000's | 79 (56.03) | 29.6817 |
| 2010's | 43 (30.50) | 24.3611 |
| 2020's | 6 (4.26) | 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% |
| Trials | 1 (0.78%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Reviews | 6 (4.65%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 20 (100.00%) | 84.16% |
| Other | 122 (94.57%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||