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Quality Control of Indolin-2-one. I found the field of Pharmacology & Pharmacy; Chemistry; Computer Science very interesting. Saw the article KinFragLib: Exploring the Kinase Inhibitor Space Using Subpocket-Focused Fragmentation and Recombination published in 2020, Reprint Addresses Volkamer, A (corresponding author), Charite, Inst Physiol, Silico Toxicol & Struct Bioinformat, D-10117 Berlin, Germany.. The CAS is 59-48-3. Through research, I have a further understanding and discovery of Indolin-2-one.

Quality Control of Indolin-2-one. I found the field of Pharmacology & Pharmacy; Chemistry; Computer Science very interesting. Saw the article KinFragLib: Exploring the Kinase Inhibitor Space Using Subpocket-Focused Fragmentation and Recombination published in 2020, Reprint Addresses Volkamer, A (corresponding author), Charite, Inst Physiol, Silico Toxicol & Struct Bioinformat, D-10117 Berlin, Germany.. The CAS is 59-48-3. Through research, I have a further understanding and discovery of Indolin-2-one.

Protein kinases play a crucial role in many cell signaling processes, making them one of the most important families of drug targets. In this context, fragment-based drug design strategies have been successfully applied to develop novel kinase inhibitors. These strategies usually follow a knowledge-driven approach to optimize a focused set of fragments to a potent kinase inhibitor. Alternatively, KinFragLib explores and extends the chemical space of kinase inhibitors using data-driven fragmentation and recombination. The method builds on available structural kinome data from the KLIFS database for over 2500 kinase DFG-in structures cocrystallized with noncovalent kinase ligands. The computational fragmentation method splits the ligands into fragments with respect to their 3D proximity to six predefined functionally relevant subpocket centers. The resulting fragment library consists of six subpocket pools with over 7000 fragments, available at https://github.com/volkamerlab/KinFragLib. KinFragLib offers two main applications: on the one hand, in-depth analyses of the chemical space of known kinase inhibitors, subpocket characteristics, and connections, and on the other hand, subpocket-informed recombination of fragments to generate potential novel inhibitors. The latter showed that recombining only a subset of 624 representative fragments generated 6.7 million molecules. This combinatorial library contains, besides some known kinase inhibitors, more than 99% novel chemical matter compared to ChEMBL and 63% molecules compliant with Lipinski’s rule of five.

About Indolin-2-one, If you have any questions, you can contact Sydow, D; Schmiel, P; Mortier, J; Volkamer, A or concate me.. Quality Control of Indolin-2-one

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An article Transition-Metal-Free Selective C(sp(3))-H Thiolation of Arylacetamides with Substituted Benzenethiols, Aryl Sulfenylchlorides and Diaryl Disulfides WOS:000524357500028 published article about S BOND FORMATION; CATALYZED C-S; SULFONYL CHLORIDES; SULFENYLATION; SULFUR; ENAMINONES; FUNCTIONALIZATION; THIOPHENOLS; SULFIDES; INDOLES in [Liu, Changying; Li, Zheyu; Weng, Zhengyun; Fang, Xinyue; Zhao, Fei; Tang, Kehui; Ma, Wenbo] Chengdu Univ, Sichuan Ind Inst Antibiot, Antibiot Res & Reevaluat Key Lab Sichuan Prov, Huaguan Rd 168, Chengdu 610052, Peoples R China; [Chen, Jianyang] Chongqing Univ Arts & Sci, Coll Chem & Environm Engn, 319 Honghe Ave, Chongqing, Peoples R China in 2020.0, Cited 60.0. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3. Name: Indolin-2-one

An article Transition-Metal-Free Selective C(sp(3))-H Thiolation of Arylacetamides with Substituted Benzenethiols, Aryl Sulfenylchlorides and Diaryl Disulfides WOS:000524357500028 published article about S BOND FORMATION; CATALYZED C-S; SULFONYL CHLORIDES; SULFENYLATION; SULFUR; ENAMINONES; FUNCTIONALIZATION; THIOPHENOLS; SULFIDES; INDOLES in [Liu, Changying; Li, Zheyu; Weng, Zhengyun; Fang, Xinyue; Zhao, Fei; Tang, Kehui; Ma, Wenbo] Chengdu Univ, Sichuan Ind Inst Antibiot, Antibiot Res & Reevaluat Key Lab Sichuan Prov, Huaguan Rd 168, Chengdu 610052, Peoples R China; [Chen, Jianyang] Chongqing Univ Arts & Sci, Coll Chem & Environm Engn, 319 Honghe Ave, Chongqing, Peoples R China in 2020.0, Cited 60.0. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3. Name: Indolin-2-one

A synthetic method for the preparation of unsymmetrical 2-arylthioacetamides though direct C(sp(3))-H thiolation of arylacetamides with readily available substituted thiols, sulfenylchlorides and disulfides have been developed. Our strategy features a green reaction medium with ample substrate scope, affording the mono-thiolated aryl acetic acid derivatives in moderate to good yields in the presence of weak bases without any transition-metal catalyst.

Name: Indolin-2-one. About Indolin-2-one, If you have any questions, you can contact Liu, CY; Li, ZY; Weng, ZY; Fang, XY; Zhao, F; Tang, KH; Chen, JY; Ma, WB or concate me.

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Recommanded Product: 59-48-3. In 2020.0 ORG LETT published article about DIRECT ARYLATION; BITHIOPHENE COPOLYMERS; CONJUGATED POLYMER; HIGH-PERFORMANCE; MATERIALS DESIGN; CONVERSION in [Nitti, Andrea; Osw, Peshawa; Calcagno, Giuseppe; Pasini, Dario] Univ Pavia, Dept Chem, I-27100 Pavia, Italy; [Nitti, Andrea; Pasini, Dario] Univ Pavia, INSTM Res Unit, I-27100 Pavia, Italy; [Osw, Peshawa] Salahaddin Univ, Coll Sci, Dept Chem, Erbil 44001, Kurdistan, Iraq; [Botta, Chiara] CNR, Ist Studio Macromol ISMAC, I-20133 Milan, Italy; [Etkind, Samuel I.; Swager, Timothy M.] MIT, Dept Chem, Cambridge, MA 02139 USA; [Bianchi, Gabriele; Po, Riccardo] Ist Donegani SpA, Res Ctr Renewable Energies & Environm, I-28100 Novara, Italy in 2020.0, Cited 43.0. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3.

Recommanded Product: 59-48-3. In 2020.0 ORG LETT published article about DIRECT ARYLATION; BITHIOPHENE COPOLYMERS; CONJUGATED POLYMER; HIGH-PERFORMANCE; MATERIALS DESIGN; CONVERSION in [Nitti, Andrea; Osw, Peshawa; Calcagno, Giuseppe; Pasini, Dario] Univ Pavia, Dept Chem, I-27100 Pavia, Italy; [Nitti, Andrea; Pasini, Dario] Univ Pavia, INSTM Res Unit, I-27100 Pavia, Italy; [Osw, Peshawa] Salahaddin Univ, Coll Sci, Dept Chem, Erbil 44001, Kurdistan, Iraq; [Botta, Chiara] CNR, Ist Studio Macromol ISMAC, I-20133 Milan, Italy; [Etkind, Samuel I.; Swager, Timothy M.] MIT, Dept Chem, Cambridge, MA 02139 USA; [Bianchi, Gabriele; Po, Riccardo] Ist Donegani SpA, Res Ctr Renewable Energies & Environm, I-28100 Novara, Italy in 2020.0, Cited 43.0. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3.

We demonstrate the broad applicability of the annulation protocol combining, in one pot, a direct arylation and cross aldol condensation for the straightforward synthesis at gram-scale of pi-extended thiophene-based scaffolds. The regiospecific direct arylation drives the subsequent cross-aldol condensation proceed under the same basic conditions, and the overall protocol has broad applicability in the synthesis of extended aromatics wherein the thiophene ring is annulated with furans, pyridines, indoles, benzothiophenes, and benzofurans. These scaffolds can be further elaborated into pi-extended, highly fluorescent oligomers with a central deficient benzothiadiazole unit with up to nine aromatic rings through coupling reactions.

Recommanded Product: 59-48-3. About Indolin-2-one, If you have any questions, you can contact Nitti, A; Osw, P; Calcagno, G; Botta, C; Etkind, SI; Bianchi, G; Po, R; Swager, TM; Pasini, D or concate me.

Reference:
Indoline – Wikipedia,
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Category: indolines-derivatives. I found the field of Biochemistry & Molecular Biology; Entomology; Physiology very interesting. Saw the article Discovery of novel indole derivatives containing dithioacetal as potential antiviral agents for plants published in 2020.0, Reprint Addresses Hu, DY; Song, BA (corresponding author), Guizhou Univ, Minist Educ, Key Lab Green Pesticide & Agr Bioengn, State Key Lab Breeding Base Green Pesticide & Agr, Guiyang 550025, Peoples R China.. The CAS is 59-48-3. Through research, I have a further understanding and discovery of Indolin-2-one.

Category: indolines-derivatives. I found the field of Biochemistry & Molecular Biology; Entomology; Physiology very interesting. Saw the article Discovery of novel indole derivatives containing dithioacetal as potential antiviral agents for plants published in 2020.0, Reprint Addresses Hu, DY; Song, BA (corresponding author), Guizhou Univ, Minist Educ, Key Lab Green Pesticide & Agr Bioengn, State Key Lab Breeding Base Green Pesticide & Agr, Guiyang 550025, Peoples R China.. The CAS is 59-48-3. Through research, I have a further understanding and discovery of Indolin-2-one.

Thirty unreported indole derivatives containing dithioacetal moiety were synthesized and evaluated for antiplant viral activity. Bioassay results displayed that some of the target compounds showed better activities against tobacco mosaic virus (TMV) than the commercial Ribavirin in vivo. In particular, anti-TMV curative, protective and inactivating activity of 4p were 55.1, 57.2, and 80.3%, respectively, and EC50 value for inactivating activity was 88.5 mu g/mL. The observation of transmission electron microscope showed that 4p may have a certain destructive effect on TMV particles. To further study, microscale thermophoresis analysis result also demonstrated that 4p powerfully interacted with TMV coat protein in vitro. Hence, this study provides a strong evidence suporting that indole derivatives might be applied as new antiviral agents.

About Indolin-2-one, If you have any questions, you can contact Wei, CL; Zhao, L; Sun, ZR; Hu, DY; Song, BA or concate me.. Category: indolines-derivatives

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Name: Indolin-2-one. In 2020.0 J FLUORESC published article about SENSOR; FE3+; PROBE; CR3+; GLYCOCLUSTER; CATIONS; AL3+ in [Sadak, Ali Enis; Karakus, Erman] TUBITAK UME Sci & Technol Res Council Turkey, Organ Chem Lab, Natl Metrol Inst, Chem Grp, TR-41470 Kocaeli, Turkey in 2020.0, Cited 36.0. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3.

Name: Indolin-2-one. In 2020.0 J FLUORESC published article about SENSOR; FE3+; PROBE; CR3+; GLYCOCLUSTER; CATIONS; AL3+ in [Sadak, Ali Enis; Karakus, Erman] TUBITAK UME Sci & Technol Res Council Turkey, Organ Chem Lab, Natl Metrol Inst, Chem Grp, TR-41470 Kocaeli, Turkey in 2020.0, Cited 36.0. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3.

We investigated the ability of a novel triazatruxene-rhodamine-based (TAT-ROD) chemosensor to detect the trivalent metal ions aluminium (Al3+), iron (Fe3+) and chromium (Cr3+). Operating via the through-bond energy transfer (TBET) pathway, the chemosensor exhibited low detection limits of 23.0, 25.0 and 170.0 nM for Al3+, Fe3+ and Cr3+, respectively, along with high sensitivity and selectivity during a brief period (<15 s). The binding ratio of the chemosensor and trivalent metal ions achieved by Job's method was 3:1, and when we added ethylenediaminetetraacetic acid (EDTA), the sensing process reversed. Altogether, our TAT-ROD chemosensor marks the first triazatruxene-based colorimetric and fluorometric metal ion sensor reported in the literature. Name: Indolin-2-one. About Indolin-2-one, If you have any questions, you can contact Sadak, AE; Karakus, E or concate me.

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I found the field of Chemistry very interesting. Saw the article Visible-light-induced ligand-free RuCl3 catalyzed C-H phosphorylation in water published in 2020.0. Name: Indolin-2-one, Reprint Addresses Liang, YM (corresponding author), Lanzhou Univ, State Key Lab Appl Organ Chem, Lanzhou 730000, Gansu, Peoples R China.. The CAS is 59-48-3. Through research, I have a further understanding and discovery of Indolin-2-one

I found the field of Chemistry very interesting. Saw the article Visible-light-induced ligand-free RuCl3 catalyzed C-H phosphorylation in water published in 2020.0. Name: Indolin-2-one, Reprint Addresses Liang, YM (corresponding author), Lanzhou Univ, State Key Lab Appl Organ Chem, Lanzhou 730000, Gansu, Peoples R China.. The CAS is 59-48-3. Through research, I have a further understanding and discovery of Indolin-2-one

Visible-light-induced C-H phosphorylation of para-C-Ar-H and heteroarenes was realized using cost-effective RuCl3 as a catalyst. The reaction conditions are green and environmentally friendly, using water as a solvent at room temperature and without ligands. A broad range of highly functional organophosphorus compounds were obtained via a cross-dehydrogenation-coupling (CDC) reaction. In addition, we also proved that RuCl3 is a photocatalyst via its absorption spectrum and on/off light experiments.

About Indolin-2-one, If you have any questions, you can contact Gou, XY; Zhang, BS; Wang, XG; Shi, WY; Liu, HC; An, Y; Zhang, Z; Liang, YM or concate me.. Name: Indolin-2-one

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I found the field of Chemistry very interesting. Saw the article Macrocyclic Modalities Combining Peptide Epitopes and Natural Product Fragments published in 2020.0. Formula: C8H7NO, Reprint Addresses Gueret, SM (corresponding author), Max Planck Inst Mol Physiol, AstraZeneca, Dept Chem Biol, Max Planck Inst Satellite Unit, D-44227 Dortmund, Germany.; Gueret, SM (corresponding author), AstraZeneca, Med Chem Res & Early Dev Cardiovasc Renal & Metab, BioPharmaceut R&D, S-43150 Gothenburg, Sweden.; Waldmann, H (corresponding author), Max Planck Inst Mol Physiol, Dept Chem Biol, D-44227 Dortmund, Germany.. The CAS is 59-48-3. Through research, I have a further understanding and discovery of Indolin-2-one

I found the field of Chemistry very interesting. Saw the article Macrocyclic Modalities Combining Peptide Epitopes and Natural Product Fragments published in 2020.0. Formula: C8H7NO, Reprint Addresses Gueret, SM (corresponding author), Max Planck Inst Mol Physiol, AstraZeneca, Dept Chem Biol, Max Planck Inst Satellite Unit, D-44227 Dortmund, Germany.; Gueret, SM (corresponding author), AstraZeneca, Med Chem Res & Early Dev Cardiovasc Renal & Metab, BioPharmaceut R&D, S-43150 Gothenburg, Sweden.; Waldmann, H (corresponding author), Max Planck Inst Mol Physiol, Dept Chem Biol, D-44227 Dortmund, Germany.. The CAS is 59-48-3. Through research, I have a further understanding and discovery of Indolin-2-one

Hot loop protein segments have variable structure and conformation and contribute crucially to protein-protein interactions. We describe a new hot loop mimicking modality, termed PepNats, in which natural product (NP)-inspired structures are incorporated as conformation-determining and-restricting structural elements into macrocyclic hot loop-derived peptides. Macrocyclic PepNats representing hot loops of inducible nitric oxide synthase (iNOS) and human agouti-related protein (AGRP) were synthesized on solid support employing macro-cyclization by imine formation and subsequent stereoselective 1,3-dipolar cycloaddition as key steps. PepNats derived from the iNOS DINNN hot loop and the AGRP RFF hot spot sequence yielded novel and potent ligands of the SPRY domain-containing SOCS box protein 2 (SPSB2) that binds to iNOS, and selective ligands for AGRP-binding melanocortin (MC) receptors. NP-inspired fragment absolute configuration determines the conformation of the peptide part responsible for binding. These results demonstrate that combination of NP-inspired scaffolds with peptidic epitopes enables identification of novel hot loop mimics with conformationally constrained and biologically relevant structure.

Formula: C8H7NO. About Indolin-2-one, If you have any questions, you can contact Gueret, SM; Thavam, S; Carbajo, RJ; Potowski, M; Larsson, N; Dahl, G; Dellsen, A; Grossmann, TN; Plowright, AT; Valeur, E; Lemurell, M; Waldmann, H or concate me.

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Recently I am researching about GAMMA-SUBSTITUTED ALLENOATES; UMPOLUNG ADDITION-REACTION; CROSS-COUPLING REACTION; MORITA-BAYLIS-HILLMAN; DIASTEREOSELECTIVE SYNTHESIS; SEQUENTIAL ANNULATION; BOND FORMATION; 3+2 CYCLOADDITION; MICHAEL ADDITION; DOMINO REACTION, Saw an article supported by the National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [21871148, 21672109, 21472097]. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Feng, JX; Huang, Y. The CAS is 59-48-3. Through research, I have a further understanding and discovery of Indolin-2-one. Name: Indolin-2-one

Recently I am researching about GAMMA-SUBSTITUTED ALLENOATES; UMPOLUNG ADDITION-REACTION; CROSS-COUPLING REACTION; MORITA-BAYLIS-HILLMAN; DIASTEREOSELECTIVE SYNTHESIS; SEQUENTIAL ANNULATION; BOND FORMATION; 3+2 CYCLOADDITION; MICHAEL ADDITION; DOMINO REACTION, Saw an article supported by the National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [21871148, 21672109, 21472097]. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Feng, JX; Huang, Y. The CAS is 59-48-3. Through research, I have a further understanding and discovery of Indolin-2-one. Name: Indolin-2-one

A phosphine-catalyzed remote 1,7-addition of vinyl allenoates has been developed, providing a series of 1,3-dienes derivatives in high yields (up to 99%) and with good chemo-, regio-, and stereoselectivity. This reaction demonstrated that the introduction of vinyl in allenoates effectively extended reaction types of phosphine-catalyzed nucleophilic addition of allenoates, leading to concise synthesis of diene carboxylates. Notably, the enantioselective variant of this 1,7-addition can also be performed by chiral phosphine catalyst.

Name: Indolin-2-one. About Indolin-2-one, If you have any questions, you can contact Feng, JX; Huang, Y or concate me.

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I found the field of Pharmacology & Pharmacy very interesting. Saw the article Identification of Small-Molecule Positive Modulators of Calcitonin-like Receptor-Based Receptors published in 2020. Name: Indolin-2-one, Reprint Addresses Hay, DL (corresponding author), Univ Auckland, Sch Biol Sci, Auckland 1010, New Zealand.; Flanagan, JU; Hay, MP; Hay, DL (corresponding author), Univ Auckland, Maurice Wilkins Ctr Mol Biodiscovery, Auckland 1010, New Zealand.; Flanagan, JU; Hay, MP (corresponding author), Univ Auckland, Auckland Canc Soc Res Ctr, Auckland 1023, New Zealand.. The CAS is 59-48-3. Through research, I have a further understanding and discovery of Indolin-2-one

I found the field of Pharmacology & Pharmacy very interesting. Saw the article Identification of Small-Molecule Positive Modulators of Calcitonin-like Receptor-Based Receptors published in 2020. Name: Indolin-2-one, Reprint Addresses Hay, DL (corresponding author), Univ Auckland, Sch Biol Sci, Auckland 1010, New Zealand.; Flanagan, JU; Hay, MP; Hay, DL (corresponding author), Univ Auckland, Maurice Wilkins Ctr Mol Biodiscovery, Auckland 1010, New Zealand.; Flanagan, JU; Hay, MP (corresponding author), Univ Auckland, Auckland Canc Soc Res Ctr, Auckland 1023, New Zealand.. The CAS is 59-48-3. Through research, I have a further understanding and discovery of Indolin-2-one

Class B G protein-coupled receptors are highly therapeutically relevant but challenges remain in identifying suitable small-molecule drugs. The calcitonin-like receptor (CLR) in particular is linked to conditions such as migraine, cardiovascular disease, and inflammatory bowel disease. The CLR cannot act as a cell-surface receptor alone but rather must couple to one of three receptor activity-modifying proteins (RAMPs), forming heterodimeric receptors for the peptides adrenomedullin and calcitonin gene-related peptide. These peptides have extended binding sites across their receptors. This is one reason why there are few small-molecule ligands that can modulate these receptors. Here we describe small molecules that are able to positively modulate the signaling of the CLR with all three RAMPs but are not active at the related calcitonin receptor. These compounds were selected from a beta-arrestin recruitment screen, coupled with rounds of medicinal chemistry to improve their activity. Translational potential is shown as the compounds can positively modulate cAMP signaling in a vascular cell line model. Binding experiments do not support an extracellular domain binding site; however, molecular modeling reveals potential allosteric binding sites in multiple receptor regions. These are the first small-molecule positive modulators described for the CLR:RAMP complexes.

Name: Indolin-2-one. About Indolin-2-one, If you have any questions, you can contact Hendrikse, ER; Liew, LP; Bower, RL; Bonnet, M; Jamaluddin, MA; Prodan, N; Richards, KD; Walker, CS; Pairaudeau, G; Smith, DM; Rujan, RM; Sudra, R; Reynolds, CA; Booe, JM; Pioszak, AA; Flanagan, JU; Hay, MP; Hay, DL or concate me.

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SDS of cas: 59-48-3. In 2020 ACS PHARMACOL TRANSL published article about GENE-RELATED PEPTIDE; CLASS-B GPCR; ACTIVITY-MODIFYING PROTEIN-2; CRYO-EM STRUCTURE; STRUCTURAL INSIGHTS; COUPLED RECEPTORS; BINDING SITES; CGRP RECEPTOR; ADRENOMEDULLIN; RECOGNITION in [Hendrikse, Erica R.; Bower, Rebekah L.; Jamaluddin, Muhammad A.; Prodan, Nicole; Richards, Keith D.; Walker, Christopher S.; Hay, Debbie L.] Univ Auckland, Sch Biol Sci, Auckland 1010, New Zealand; [Hendrikse, Erica R.; Bower, Rebekah L.; Jamaluddin, Muhammad A.; Walker, Christopher S.; Flanagan, Jack U.; Hay, Michael P.; Hay, Debbie L.] Univ Auckland, Maurice Wilkins Ctr Mol Biodiscovery, Auckland 1010, New Zealand; [Liew, Lydia P.; Bonnet, Muriel; Flanagan, Jack U.; Hay, Michael P.] Univ Auckland, Auckland Canc Soc Res Ctr, Auckland 1023, New Zealand; [Pairaudeau, Garry] AstraZeneca, Hit Discovery, Discovery Sci, R&D, Cambridge CB2 0SL, England; [Smith, David M.] AstraZeneca, Emerging Innovat, R&D, Discovery Sci, Cambridge CB2 0SL, England; [Rujan, Roxana-Maria; Sudra, Risha; Reynolds, Christopher A.] Univ Essex, Sch Life Sci, Colchester CO4 3SQ, Essex, England; [Booe, Jason M.; Pioszak, Augen A.] Univ Oklahoma, Dept Biochem & Mol Biol, Hlth Sci Ctr, Oklahoma City, OK 73104 USA in 2020, Cited 67. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3.

SDS of cas: 59-48-3. In 2020 ACS PHARMACOL TRANSL published article about GENE-RELATED PEPTIDE; CLASS-B GPCR; ACTIVITY-MODIFYING PROTEIN-2; CRYO-EM STRUCTURE; STRUCTURAL INSIGHTS; COUPLED RECEPTORS; BINDING SITES; CGRP RECEPTOR; ADRENOMEDULLIN; RECOGNITION in [Hendrikse, Erica R.; Bower, Rebekah L.; Jamaluddin, Muhammad A.; Prodan, Nicole; Richards, Keith D.; Walker, Christopher S.; Hay, Debbie L.] Univ Auckland, Sch Biol Sci, Auckland 1010, New Zealand; [Hendrikse, Erica R.; Bower, Rebekah L.; Jamaluddin, Muhammad A.; Walker, Christopher S.; Flanagan, Jack U.; Hay, Michael P.; Hay, Debbie L.] Univ Auckland, Maurice Wilkins Ctr Mol Biodiscovery, Auckland 1010, New Zealand; [Liew, Lydia P.; Bonnet, Muriel; Flanagan, Jack U.; Hay, Michael P.] Univ Auckland, Auckland Canc Soc Res Ctr, Auckland 1023, New Zealand; [Pairaudeau, Garry] AstraZeneca, Hit Discovery, Discovery Sci, R&D, Cambridge CB2 0SL, England; [Smith, David M.] AstraZeneca, Emerging Innovat, R&D, Discovery Sci, Cambridge CB2 0SL, England; [Rujan, Roxana-Maria; Sudra, Risha; Reynolds, Christopher A.] Univ Essex, Sch Life Sci, Colchester CO4 3SQ, Essex, England; [Booe, Jason M.; Pioszak, Augen A.] Univ Oklahoma, Dept Biochem & Mol Biol, Hlth Sci Ctr, Oklahoma City, OK 73104 USA in 2020, Cited 67. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3.

Class B G protein-coupled receptors are highly therapeutically relevant but challenges remain in identifying suitable small-molecule drugs. The calcitonin-like receptor (CLR) in particular is linked to conditions such as migraine, cardiovascular disease, and inflammatory bowel disease. The CLR cannot act as a cell-surface receptor alone but rather must couple to one of three receptor activity-modifying proteins (RAMPs), forming heterodimeric receptors for the peptides adrenomedullin and calcitonin gene-related peptide. These peptides have extended binding sites across their receptors. This is one reason why there are few small-molecule ligands that can modulate these receptors. Here we describe small molecules that are able to positively modulate the signaling of the CLR with all three RAMPs but are not active at the related calcitonin receptor. These compounds were selected from a beta-arrestin recruitment screen, coupled with rounds of medicinal chemistry to improve their activity. Translational potential is shown as the compounds can positively modulate cAMP signaling in a vascular cell line model. Binding experiments do not support an extracellular domain binding site; however, molecular modeling reveals potential allosteric binding sites in multiple receptor regions. These are the first small-molecule positive modulators described for the CLR:RAMP complexes.

SDS of cas: 59-48-3. About Indolin-2-one, If you have any questions, you can contact Hendrikse, ER; Liew, LP; Bower, RL; Bonnet, M; Jamaluddin, MA; Prodan, N; Richards, KD; Walker, CS; Pairaudeau, G; Smith, DM; Rujan, RM; Sudra, R; Reynolds, CA; Booe, JM; Pioszak, AA; Flanagan, JU; Hay, MP; Hay, DL or concate me.

Reference:
Indoline – Wikipedia,
,Indoline | C8H9N – PubChem