| Assay ID | Title | Year | Journal | Article |
|---|
| AID538471 | Metabolic stability in human liver microsomes assessed as half life | 2010 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
| Synthesis and SAR of 4-aryl-1-(indazol-5-yl)pyridin-2(1H)ones as MCH-1 antagonists for the treatment of obesity. |
| AID538476 | Reduction in body weight in diet induced obese C57BL/6J mouse at 10 mg/kg, po qd | 2010 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
| Synthesis and SAR of 4-aryl-1-(indazol-5-yl)pyridin-2(1H)ones as MCH-1 antagonists for the treatment of obesity. |
| AID538466 | Inhibition of CYP3A4 | 2010 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
| Synthesis and SAR of 4-aryl-1-(indazol-5-yl)pyridin-2(1H)ones as MCH-1 antagonists for the treatment of obesity. |
| AID538472 | Metabolic stability in rat liver microsomes assessed as half life | 2010 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
| Synthesis and SAR of 4-aryl-1-(indazol-5-yl)pyridin-2(1H)ones as MCH-1 antagonists for the treatment of obesity. |
| AID1233425 | Plasma concentration in Sprague-Dawley rat at 15 mg/kg, po qd measured at 20 hrs post dose | 2015 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 25, Issue:14
| Dihydropyrrolopyrazol-6-one MCHR1 antagonists for the treatment of obesity: Insights on in vivo efficacy from a novel FLIPR assay setup. |
| AID538467 | Inhibition of CYP1A2 | 2010 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
| Synthesis and SAR of 4-aryl-1-(indazol-5-yl)pyridin-2(1H)ones as MCH-1 antagonists for the treatment of obesity. |
| AID1319405 | Displacement of [Phe13,125I]Tyr19]-MCH from human MCHR1 E4Q/A5T double mutant expressed in HEK293 cells by TopCount scintillation counting method | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
| Synthesis and Antiobesity Properties of 6-(4-Chlorophenyl)-3-(4-((3,3-difluoro-1-hydroxycyclobutyl)methoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-one (BMS-814580): A Highly Efficacious Melanin Concentrating Hormone Receptor 1 (MCHR1) Inhibitor. |
| AID1233431 | Drug uptake in Sprague-Dawley rat brain at 15 mg/kg, po qd measured at 20 hrs post dose | 2015 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 25, Issue:14
| Dihydropyrrolopyrazol-6-one MCHR1 antagonists for the treatment of obesity: Insights on in vivo efficacy from a novel FLIPR assay setup. |
| AID538464 | Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells | 2010 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
| Synthesis and SAR of 4-aryl-1-(indazol-5-yl)pyridin-2(1H)ones as MCH-1 antagonists for the treatment of obesity. |
| AID1233402 | Lipophilicity, log P of the compound by HPLC analysis | 2015 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 25, Issue:14
| Dihydropyrrolopyrazol-6-one MCHR1 antagonists for the treatment of obesity: Insights on in vivo efficacy from a novel FLIPR assay setup. |
| AID1233401 | Displacement of [Phe13, [125I]Tyr19]-MCH from human MCHR1 E4Q/A5T double mutant expressed in HEK293 cell membranes after 90 mins by scintillation counting analysis | 2015 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 25, Issue:14
| Dihydropyrrolopyrazol-6-one MCHR1 antagonists for the treatment of obesity: Insights on in vivo efficacy from a novel FLIPR assay setup. |
| AID1454462 | Displacement of [3H]-N-alpha-methylhistamine from human H3R expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis | 2017 | ACS medicinal chemistry letters, Jun-08, Volume: 8, Issue:6
| Systematic Data Mining Reveals Synergistic H3R/MCHR1 Ligands. |
| AID538470 | Inhibition of CYP2D6 | 2010 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
| Synthesis and SAR of 4-aryl-1-(indazol-5-yl)pyridin-2(1H)ones as MCH-1 antagonists for the treatment of obesity. |
| AID1233437 | Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay | 2015 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 25, Issue:14
| Dihydropyrrolopyrazol-6-one MCHR1 antagonists for the treatment of obesity: Insights on in vivo efficacy from a novel FLIPR assay setup. |
| AID538474 | Aqueous solubility of the compound in phosphate buffer at pH 7.4 | 2010 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
| Synthesis and SAR of 4-aryl-1-(indazol-5-yl)pyridin-2(1H)ones as MCH-1 antagonists for the treatment of obesity. |
| AID353589 | Displacement of [3H]astemizole from human ERG expressed in HEK293 cells | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
| Novel approach for chemotype hopping based on annotated databases of chemically feasible fragments and a prospective case study: new melanin concentrating hormone antagonists. |
| AID1233413 | Antiobesity activity in Sprague-Dawley rat assessed as body weight loss at 15 mg/kg, po qd administered 1 hr prior to onset of dark cycle measured for 7 days relative to vehicle-treated control | 2015 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 25, Issue:14
| Dihydropyrrolopyrazol-6-one MCHR1 antagonists for the treatment of obesity: Insights on in vivo efficacy from a novel FLIPR assay setup. |
| AID538465 | Inhibition of CYP2C19 | 2010 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
| Synthesis and SAR of 4-aryl-1-(indazol-5-yl)pyridin-2(1H)ones as MCH-1 antagonists for the treatment of obesity. |
| AID538468 | Inhibition of CYP2B6 | 2010 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
| Synthesis and SAR of 4-aryl-1-(indazol-5-yl)pyridin-2(1H)ones as MCH-1 antagonists for the treatment of obesity. |
| AID270769 | Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay | 2006 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
| The discovery and optimization of pyrimidinone-containing MCH R1 antagonists. |
| AID353586 | Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
| Novel approach for chemotype hopping based on annotated databases of chemically feasible fragments and a prospective case study: new melanin concentrating hormone antagonists. |
| AID538469 | Inhibition of CYP2C9 | 2010 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
| Synthesis and SAR of 4-aryl-1-(indazol-5-yl)pyridin-2(1H)ones as MCH-1 antagonists for the treatment of obesity. |
| AID443384 | Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay | 2009 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21
| Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation. |
| AID1233403 | Inhibition of human ERG expressed in CHO cells at 0.3 uM by automated whole-cell patch clamp electrophysiology system relative to control | 2015 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 25, Issue:14
| Dihydropyrrolopyrazol-6-one MCHR1 antagonists for the treatment of obesity: Insights on in vivo efficacy from a novel FLIPR assay setup. |
| AID1319497 | Inhibition of human ERG at 1 uM by patch clamp assay | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
| Synthesis and Antiobesity Properties of 6-(4-Chlorophenyl)-3-(4-((3,3-difluoro-1-hydroxycyclobutyl)methoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-one (BMS-814580): A Highly Efficacious Melanin Concentrating Hormone Receptor 1 (MCHR1) Inhibitor. |
| AID1233419 | Fraction unbound in Sprague-Dawley rat plasma at 15 mg/kg, po qd | 2015 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 25, Issue:14
| Dihydropyrrolopyrazol-6-one MCHR1 antagonists for the treatment of obesity: Insights on in vivo efficacy from a novel FLIPR assay setup. |
| AID1233436 | Ratio of unbound concentration in Sprague-Dawley rat brain at 15 mg/kg, po qd to Ki for rat MCHR1 | 2015 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 25, Issue:14
| Dihydropyrrolopyrazol-6-one MCHR1 antagonists for the treatment of obesity: Insights on in vivo efficacy from a novel FLIPR assay setup. |
| AID1233406 | Antagonist activity at rat MCHR1 | 2015 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 25, Issue:14
| Dihydropyrrolopyrazol-6-one MCHR1 antagonists for the treatment of obesity: Insights on in vivo efficacy from a novel FLIPR assay setup. |
| AID538473 | Metabolic stability in mouse liver microsomes assessed as half life | 2010 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
| Synthesis and SAR of 4-aryl-1-(indazol-5-yl)pyridin-2(1H)ones as MCH-1 antagonists for the treatment of obesity. |
| AID1319450 | Binding affinity to rat MCHR1 | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
| Synthesis and Antiobesity Properties of 6-(4-Chlorophenyl)-3-(4-((3,3-difluoro-1-hydroxycyclobutyl)methoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-one (BMS-814580): A Highly Efficacious Melanin Concentrating Hormone Receptor 1 (MCHR1) Inhibitor. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1346168 | Human MCH1 receptor (Melanin-concentrating hormone receptors) | 2006 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
| The discovery and optimization of pyrimidinone-containing MCH R1 antagonists. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |